Erik De Clercq

A lengendary physician, scientist, professor and father!

Erik De Clercq

M.D. Ph.D. Erik De Clercq is a professor emeritus at the KU Leuven, Belgium, and a visiting professor at the University of South Bohemia in the Czech Republic. His research interests are embraced within the broad areas of microbiology, virology, molecular biology and antiviral research, focusing on HIV, HBV, HCV, influenza, VZV, herpesvirus and merging viruses (e.g. Ebola, Dengue, Chikungunya). Over a period of five decades, he has developed new antiviral medicines include nucleotide analogues (e.g. tenofovir), and he has co-invented several approved antiviral drugs such as BVDU (brivudin), amino acyl esters of acyclovir (e.g. valaciclovir), acyclic nucleoside phosphonates (ANPs, cidofovir, adefovir, tenofovir), non-nucleoside reverse transcriptase inhibitors, HEPT and TIBO derivatives leading to rilpivirine for the treatment of AIDS. Since the start of his academic career in 1967, Prof. Erik De Clercq has published more than 2700 research articles.

My curriculum vitae (CV)

Current affiliation: Rega Institute for Medical Research, Department of Microbiology and Immunology, KU Leuven - University of Leuven, Leuven, Belgium

Email: Erik.DeClercq@rega.kuleuven.be

Key events of my life

22 publications in the year 2016



1. Neca, J., Kastl, T., Palus, M., De Clercq, E., Eyer, L., Nencka, R. & Šmidková, M.
   Structure-activity relationships of nucleoside analogues for inhibition of tick-borne encephalitis virus.
   Antiviral Res., in press (2016).
   


2. Eyer, L., Nencka, R., Huvarová, I., Palus, M., Alves, M.J., Niedrig, M., Gould, E.A., De Clercq, E. & Růžek, D.
   Nucleoside inhibitors of Zika virus and their structure-activity relationships.
   J. Infect. Dis., in press (2016).
   


3. De Clercq, E.
   Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF).
   Biochem. Pharmacol., in press (2016).
   


4. Li, W., Huang, B., Kang, D., De Clercq, E., Daelemans, D., Pannecouque, C., Zhan, P. & Liu, X.
   Design, synthesis and biological evaluation of novel 5-alkyl-6-adamantylmethylpyrimidin-4(3H)-ones as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
   Chem. Biol. Drug Des., in press (2016).
   


5. Singh Bhadauria, V., Sravanthi, V., Kumar, S., Das, D., De Clercq, E., Schols, D., Tokuda, H. & Karki, S.S.
   Synthesis and cytotoxic evaluation of some 2-{4-[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]phenoxy}-N-phenylacetamide.
   Acta Pol. Pharm. - Drug Res., in press (2016).
   


6. Panda, A.K., Das, U., Sakagami, H., Kawase, M., Balzarini, J., De Clercq, E. & Dimmock, J.R.
   Niacin esters of chalcones with tumour-selective properties.
   J. Enzyme Inhib. Med. Chem., in press (2016).
   


7. Li, X., Huang, B., Zhou, Z., Gao, P., Pannecouque, C., Daelemans, D., De Clercq, E., Zhan, P. & Liu, X.
   Arylazolyl(azinyl)thioacetanilides. Part 19: Discovery of novel substituted imidazo[4,5-b]pyridin-2-ylthioacetanilides as potent HIV NNRTIs via a structure-based bioisosterism approach.
   Chem. Biol. Drug Des., 88: 241-253 (2016).
   


8. Katiyar, A., Metikurki, B., Prafulla, S., Kumar, S., Kushwaha, S., Schols, D., De Clercq, E. & Karki, S.S
   Synthesis and pharmacological activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives.
   Acta Pol. Pharm. – Drug Res., 73, 937-947 (2016).
   


9. Kumar, S., Metikurki, B., Bhadauria, V.S., De Clercq, E., Schols, D., Tokuda, H. & Karki, S.S.
   Synthesis of imidazo[2,1-b][1,3,4]thiadiazole derivatives as possible biologically active agents.
   Acta Pol. Pharm. – Drug Res., 73: 913-929 (2016).
   


10. Li, G. & De Clercq, E.
    HIV genome-wide protein associations: a review of 30 years of research.
    Microbiol. Mol. Biol. Rev., 80: 679-731 (2016).
    
    
    
    


11. De Clercq, E. & Li, G.
    Approved antiviral drugs over the past 50 years.
    Clin. Microbiol. Rev., 29: 695-747 (2016).
    
    
    
    


12. Tatar, E., Şenkardeş, S., Sellitepe, H.E., Küçükgüzel, S.G., Karaoğlu, S.A., Bozdeveci, A., De Clercq, E., Pannecouque, C., Hadda, T.B. & Küçükgüzel, I.
    Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from N-(arylsulfonyl)methionine.
    Turkish J. Chem., 40: 510-534 (2016).
    


13. Chen, W., Zhan, P., Daelemans, D., Yang, J., Huang, B., De Clercq, E., Pannecouque, C. & Liu, X.
    Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
    Eur. J. Med. Chem., 121: 352-363 (2016).
    


14. Kulabaş, N., Tatar, E., Özakpınar, O.B., Özsavcı, D., Pannecouque, C., De Clercq, E. & Küçükgüzel, I.
    Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.
    Eur. J. Med. Chem., 121, 58-70 (2016).
    


15. Hossain, M., Das, U., Umemura, N., Sakagami, H., Balzarini, J., De Clercq E., Kawase, M. & Dimmock, J.R.
    Tumour-specific cytotoxicity and structure-activity relationships of novel 1-[3-(2-methoxyethylthio)propionyl]-3,5-bis(benzylidene)-4-piperidones.
    Bioorg. Med. Chem., 24: 2206-2214 (2016).
    


16. Zhan, P., Pannecouque, C., De Clercq, E. & Liu, X.
    Anti-HIV drug discovery and development: current innovations and future trends.
    J. Med. Chem., 59: 2849-2878 (2016).
    


17. Tatar, E., Karakuş, S., Küçükgüzel, S.G., Öktem Okullu, S., Ünübol, N., Kocagöz, T., De Clercq, E., Andrei, G., Snoeck, R., Pannecouque, C., Kalaycı, S., Şahin, F., Sriram, D., Yogeeswari, P. & Küçükgüzel, I.
    Design, synthesis, and molecular docking studies of a conjugated thiadiazole-thiourea scaffold as antituberculosis agents.
    Biol. Pharm. Bull., 39: 502-515 (2016).
    


18. De Clercq, E.
    C-nucleosides to be revisited.
    J. Med. Chem., 59: 2301-2311 (2016).
    


19. Meng, Q., Chen, X., Kang, D., Huang, B., Li, W., Zhan, P., Daelemans, D., De Clercq, E., Pannecouque, C. & Liu, X.
    Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
    Eur. J. Med. Chem., 115: 53-62 (2016).
    


20. Karki, S.S., Das, U., Umemura, N., Sakagami, H., Iwamoto, S., Kawase, M., Balzarini, J., De Clercq, E., Dimmock, S.G. & Dimmock, J.R.
    3,5-Bis(3-alkylaminomethyl-4-hydroxybenzylidene)-4-piperidones: a novel class of potent tumor-selective cytotoxins.
    J. Med. Chem., 59: 763–769 (2016).
    


21. Yang, J., Chen, W., Kang, D., Lu, X., Li, X., Liu, Z., Huang, B., Daelemans, D., Pannecouque, C., De Clercq, E., Zhan, P. & Liu, X.
    Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
    Eur. J. Med. Chem., 109: 294-304 (2016).
    


22. Huang, B., Li, X., Zhan, P., De Clercq, E., Daelemans, D., Pannecouque, C. & Liu, X.
    Design, synthesis, and biological evaluation of novel 2-(pyridin-3-yloxy)acetamide derivatives as potential anti-HIV-1 agents.
    Chem. Biol. Drug Des., 87: 283-289 (2016).
    



29 publications in the year 2015



23. De Clercq, E.
    An Odyssey in antiviral drug development – 50 years at the Rega Institute: 1964-2014.
    Acta Pharm. Sinica B, 5: 520-543 (2015).
    


24. De Clercq, E.
    Curious (old and new) antiviral nucleoside analogues with intruiging therapeutic potential.
    Curr. Med. Chem., 22: 3866-3880 (2015).
    


25. De Clercq, E.
    Current treatment of hepatitis B virus infections.
    Rev. Med. Virol., 25: 354-365 (2015).
    


26. Gu, S.-X., Qiao, H., Zhu, Y.-Y., Shu, Q.-C., Liu, H., Ju, X.-L., De Clercq, E., Balzarini, J. & Pannecouque, C.
    A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
    Bioorg. Med. Chem., 23: 6587-6593 (2015).
    


27. Fang, Z., Kang, D., Zhang, L., Huang, B., Liu, H., Pannecouque, C., De Clercq, E., Zhan, P. & Liu, X.
    Synthesis and biological evaluation of a series of 2-((1-substituted-1H-1,2,3-triazol-4-yl)methylthio)-6-(naphthalen-1-ylmethyl)pyrimidin-4(3H)-one as potential HIV-1 inhibitors.
    Chem. Biol. Drug Des., 86: 614-618 (2015).
    


28. Kang D.,, Fang, Z., Huang, B., Zhang, L., Liu, H., Pannecouque, C., Naesens; L., De Clercq, E., Zhan, P. & Liu, X.
    Synthesis and preliminary antiviral activities of piperidine-substituted purines against HIV and influenza A/H1N1 infections.
    Chem. Biol. Drug Des., 86: 568-577 (2015).
    


29. Tatar, E., Küçükgüzel, S.G., Karakuş, S., De Clercq, E., Andrei, G., Snoeck, R., Pannecouque, C., Öktem Okullu, S., Ünübol, N., Kocagöz, T., Kalaycı, S., Şahin, F. & Küçükgüzel, I.
    Synthesis and biological evaluation of some new 1,3,4-thiadiazole and 1,2,4-triazole derivatives from L-methionine as antituberculosis and antiviral agents.
    Marmara Pharm. J., 19: 88-102 (2015).
    


30. Zhang, L., Guo, J., Liu, X., Liu, H., De Clercq, E., Pannecouque, C. & Liu, X.
    Design, synthesis, and biological evaluation of novel benzoyl diarylamine/ether derivatives as potential anti-HIV-1 agents.
    Chem. Biol. Drug Des., 86: 333-343 (2015).
    


31. Wan, Z.-Y., Yao, J., Mao, T.-Q., Wang, X.-L., Wang, H.-F., Chen, W.-X., Yin, H., Chen, F.-E., De Clercq, E., Daelemans, D. & Pannecouque, C.
    Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
    Eur. J. Med. Chem., 102: 215-222 (2015).
    


32. Eyer, L., Valdés, J.J., Gil, V.A., Nencka, R., Hřebabecký, H., Šála, M., Salát,J., Černý, J., Palus, M., De Clercq, E. & Růžek, D.
    Nucleoside inhibitors of tick-borne encephalitis virus.
    Antimicrob. Agents Chemother., 59: 5483-5493 (2015).
    


33. Li, W., Li, X., De Clercq, E., Zhan, P. & Liu, X.
    Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors from arylthioacetanilide structural motif.
    Eur. J. Med. Chem., 102: 167-179 (2015).
    


34. Wan, Z.-Y., Tao, Y., Wang, Y.-F., Mao, T.-Q., Yin, H., Chen, F.-E., Piao, H.-R., De Clercq, E., Daelemans, D. & Pannecouque, C.
    Hybrid chemistry. Part 4: Discovery of etravirine–VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
    Bioorg. Med. Chem., 23: 4248-4255 (2015).
    


35. De Clercq, E.
    Development of antiviral drugs for the treatment of hepatitis C at an accelerating pace.
    Rev. Med. Virol., 25: 254-267 (2015).
    


36. Chen, X., Meng, Q., Qiu, L., Zhan, P., Liu, H., De Clercq, E., Pannecouque, C. & Liu, X.
    Design, synthesis and anti-HIV evaluation of novel triazine derivatives targeting the entrance channel of NNRTI binding pocket.
    Chem. Biol. Drug Des., 86: 902-908 (2015).
    


37. Liu, T., Huang, B., Tian, Y., Liang, X., Liu, H., Liu, H., Zhan, P., De Clercq, E., Pannecouque, C. & and Liu, X.
    Design, synthesis, and biological evaluation of novel 4-aminopiperidinyl-linked 3,5-disubstituted-1,2,6-thiadiazine-1,1-dione derivatives as HIV-1 NNRTIs.
    Chem. Biol. Drug Des., 86: 887-893 (2015).
    


38. Rai, D., Wang, L., Jiang, X., Zhan, P., Jia, H., De Clercq, E. & Liu, X.
    The changing face of hepatitis C: Recent advances on HCV inhibitors targeting NS5A.
    Curr. Med. Chem., 22: 1860-1879 (2015).
    


39. De Clercq, E.
    Curious discoveries in antiviral drug development: The role of serendipity.
    Med. Res. Rev., 35: 698-719 (2015).
    


40. De Clercq, E.
    AMD3100/CXCR4 inhibitor.
    Front. Immunol., 6: 276 (2015).
    


41. Mao, T.-Q., He, Q.-Q., Wan, Z.-Y., Chen, W.-X., Chen, F.-E., Tang, G.-F., De Clercq, E., Daelemans, D. & Pannecouque, C.
    Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
    Bioorg. Med. Chem., 23: 3860-3868 (2015).
    


42. Katiyar, A., Hegde, M., Kumar, S., Gopalakrishnan, V., Bhatelia, K.D., Ananthaswamy, K., Ramareddy, S.A., De Clercq, E., Choudhary, B., Schols, D., Raghavan, S.C. & Karki, S.S.
    Synthesis and evaluation of the biological activity of N'-[2-oxo-1,2-dihydro-3H-indol-3-ylidene]benzohydrazides as potential anticancer agents.
    RSC Adv., 5: 45492-45501 (2015).
    


43. Wan, Z.-Y., Yao, J., Tao, Y., Mao, T.-Q., Wang, X.-L., Lu, Y.-P., Wang, H.-F., Yin, H., Wu, Y., Chen, F.-E., De Clercq, E., Daelemans, D. & Pannecouque, C.
    Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
    Eur. J. Med. Chem., 97: 1-9 (2015).
    


44. De Clercq, E.
    Vesicular stomatitis virus (VSV) as a paradigm for predicting antiviral activity against Ebola virus (EBOV).
    Marmara Pharm. J., 19: 141-152 (2015).
    


45. De Clercq, E.
    Chemotherapy of respiratory syncytial virus (RSV) infections: the final breakthrough.
    Int. J. Antimicrob. Chemother., 45: 234-237 (2015).
    


46. Huang, B., Liang, X., Li, C., Chen, W., Liu, T., Li, X., Sun, Y., Fu, L., Liu, H., De Clercq, E., Pannecouque, C., Zhan, P. & Liu, X..
    Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: Design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
    Eur. J. Med. Chem., 93: 330-337 (2015).
    


47. Huang, B., Li, C., Chen, W., Liu, T., Yu, M., Fu, L., Sun, Y., Liu, H., De Clercq, E., Pannecouque, C., Zhan, P. & Liu, X.
    Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches
    Eur. J. Med. Chem., 92: 754-765 (2015).
    


48. Wu, H.-Q., Jao, J., He, Q.-Q., Chen, W.-X., Chen, F.-E., Pannecouque, C., De Clercq, E. & Daelemans, D.
    Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
    Bioorg. Med. Chem., 23: 624-631 (2015).
    


49. Gu, S.-X., Zhu, Y.-Y., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
    Structural modification of diarylpyrimidine derivatives as HIV-1 reverse transcriptase inhibitors.
    Med. Chem. Res., 24: 220-22 (2015).
    


50. De Clercq E.
    Ebola virus (EBOV) infection: therapeutic strategies.
    Biochem. Pharmacol., 93: 1-10 (2015).
    


51. Romero, M, Zanuy, M., Rosell, E., Cascante, M., Piulats, J., Font-Bardia, M., Balzarini, J., De Clercq; E. & Pujol, M.D.
    Optimization of xanthatin extraction from Xanthium spinosum L. and its cytotoxic, anti-angiogenesis and antiviral properties.
    Eur. J. Med. Chem., 90: 491-496 (2015).
    



28 publications in the year 2014



52. Patel, P.K., Patel, R.V., Mahajan, D.H., Parikh, P.A., Mehta, G.N., Pannecouque, C., De Clercq, E. & Chikhalia, K.H.
    Different heterocycles functionalized s-triazine analogues: Design, synthesis and in vitro antimicrobial, antituberculosis, and anti-HIV assessment.
    J. Heterocyclic Chem., 51: 1641-1658 (2014).
    


53. Karki, S.S., Ravikumr, T.K., R., Khatiyar, A., Thota, S., Kumar, S., Ramareddy, S.A., De Clercq, E. & Balzarini, J.
    Synthesis, cytostatic and antiviral activity of some ruthenium (II) complexes.
    Turk. J. Pharm. Sci., 11: 163-174 (2014).
    


54. Wang, J., Wang, Y., Li, Z. Zhan, P., Bai, R., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
    Design, synthesis and biological evaluation of substituted guanidine indole derivatives as potential inhibitors of HIV-1 Tat-TAR interaction.
    Med. Chem., 10: 738-746 (2014).
    


55. Rai, D., Chen, W., Zhan, P., Liu, H., Tian, Y., Liang, X., De Clercq, E., Pannecouque, C., Balzarini J. & Liu, X.
    Synthesis and anti-HIV activity of 4-(naphthalen-1-yl)-1,2,5-thiadiazol-3- hydroxyl derivatives.
    Chem. Biol. Drug Des., 84: 420-430 (2014).
    


56. Liu, Z., Chen, W., Zhan, P., De Clercq, E., Pannecouque, C. & Liu, X.
    Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
    Eur. J. Med. Chem., 87: 52-62 (2014).
    


57. Liu, T., Huang, B., Zhan, P., De Clercq, E. & Liu, X.
    Discovery of small molecular inhibitors targeting HIV-1 gp120-CD4 interaction drived from BMS-378806.
    Eur. J. Med. Chem., 86: 481-490 (2014).
    


58. Li, X., Lu, X., Chen, W., Liu, H., Zhan, P., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
    Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
    Bioorg. Med. Chem., 22: 5290-5297 (2014).
    


59. Asundaria, S.T., Pannecouque, C., De Clercq, E. & Patel, K.C.
    Sydnone sulfonamide derivatives as antibacterial, antifungal, antiproliferative and anti-HIV agents.
    Pharm. Chem. J., 48: 260-268 (2014).
    


60. Wang, L., Tian, Y., Chen, W., Liu, H., Zhan, P., Li, D., Liu, H., De Clercq, E., Pannecouque, C. & Liu, X.
    Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2. Discovery of novel [1,2,4]triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
    Eur. J. Med. Chem., 85: 293-303 (2014).
    


61. Kumar, M., Ramasamy, K., Mani. V., Mishra, R.K., Majeed, A.B.A., De Clercq, E. & Narasimhan, B.
    Synthesis, antimicrobial, anticancer, antiviral evaluation and QSAR studies of 4-(1-aryl-2-oxo-1,2-dihydro-indol-3-ylideneamino)-N-substituted benzene sulfonamides.
    Arabian J. Chem., 7: 396-408 (2014).
    


62. Kumar, S., Hegde, M., Gopalakrishnan, V., Renuka, V.K., Ramareddy, S.A., De Clercq, E., Schols, D., Gudibabande Narasimhamurthy, A.K., Raghavan, S.C. & Karki, S.S..
    2-(4-Chlorobenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazoles: synthesis, cytotoxic activity and mechanism of action.
    Eur. J. Med. Chem., 84: 687-697 (2014).
    


63. De Clercq, E.
    Sofosbuvir in the current context of hepatitis C treatment
    J. Symptoms and Signs, 3: 126-131 (2014).
    


64. Liu, Y., Meng, G., Zheng, A., Chen, F., Chen, W., De Clercq, E., Pannecouque, C. & Balzarini, J.
    Design and synthesis of a new series of cyclopropylamino-linking diarylpyrimidines as HIV non-nucleoside reverse transcriptase inhibitors.
    Eur. J. Pharm. Sci., 62: 334-341 (2014).
    


65. Meng, G., Liu, Y., Zheng, A., Chen, F., Chen, W., De Clercq, E., Pannecouque, C. & Balzarini, J.
    Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
    Eur. J. Med. Chem., 82: 600-611 (2014).
    


66. De Clercq, E.
    Current race in the development of DAAs (direct-acting antivirals) against HCV.
    Biochem. Pharmacol., 89: 441-452 (2014).
    


67. Yan, Z.-H., Wu, H.-Q., Chen, W.-X., Wu, Y., Piao, H.-R., He, Q.-Q., Chen, F.-E., De Clercq, E. & Pannecouque, C.
    Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors
    Bioorg. Med. Chem., 22: 3220-3226 (2014).
    


68. Wu, H.-Q., Pannecouque, C., Yan, Z.-H., Chen, W.-X., He, Q.-Q., Chen, F.-E., Balzarini, J., Daelemans, D. & De Clercq, E.
    Synthesis and biological evaluation of new conformationally restricted S-DABO hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
    Med. Chem.Comm., 5: 468-473 (2014).
    


69. Basarić, N., Sohora, M., Cindro, N., Mlinarić-Majerski, K., De Clercq, E. & Balzarini, J.
    Antiproliferative and antiviral activity of three libraries of adamantane derivatives.
    Arch. Pharm. Chem. Life Sci., 347: 334-340 (2014).
    


70. Li, X., Chen, W., Tian, Y., Liu, H., Zhan, P., De Clercq, E., Pannecouque, C., Balzarini, J. & Liu, X.
    Discovery of novel diarylpyrimidines as potent HIV NNRTIs via a structure-guided core-refining approach.
    Eur. J. Med. Chem., 80: 112-121 (2014).
    


71. Cao, L., Song, W., Zhan, P., Weiguo, S., De Clercq, E. & Liu, X.
    Recent progress in the research of small molecule HIV-1 RNase H inhibitors.
    Curr. Med. Chem., 21: 1956-1967 (2014).
    


72. Yan, Z.-H., Huang, X.-Y., Wu, H.-Q., Chen, W.-X., He, Q.-Q., Chen, F.-E., De Clercq, E. & Pannecouque, C.
    Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
    Bioorg. Med. Chem., 22: 2535-2541 (2014).
    


73. Tian, Y., Du, D., Rai, D., Wang, L., Liu, H., Zhan, P., De Clercq, E., Pannecouque, C. & Liu, X.
    Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: Design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
    Bioorg. Med. Chem., 22: 2052-2059 (2014).
    


74. Santiago-Vazquez, Y., Das, S., Das, U., Robles-Escajeda, E., Ortega, N.M., Lema, C., Varela-Ramirez, A., Aguilera, R.J., Balzarini, J., De Clercq, E., Dimmock, S.G., Gorecki, D.K.J. & Dimmock, J.R.
    Novel 3,5-bis(arylidene)-4-oxo-1-piperidinyl dimers: structure-activity relationships and potent antileukemic and antilymphoma cytotoxicity.
    Eur. J. Med. Chem., 77: 315-322 (2014).
    


75. Wang, J., Zhan, P., Li, Z., Liu, H., De Clercq, E., Pannecouque, C. & Liu, X.
    Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
    Eur. J. Med. Chem., 76: 531-538 (2014).
    


76. Chen, W., Zhan, P., Rai, D., De Clercq, E., Pannecouque, C., Balzarini, J., Zhou, Z., Liu, H. & Liu, X.
    Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
    Bioorg. Med. Chem., 22: 1863-1872 (2014).
    


77. Modh, R.P., De Clercq, E., Pannecouque, C. & Chikhalia, K.H.
    Design, synthesis, antimicrobial activity and anti-HIV activity evaluation of novel hybrid quinazoline-triazine derivatives.
    J. Enzyme Inhib. Med. Chem., 29: 100-108 (2014).
    


78. Gangarapu, K., Manda, S., Jallapally, A., Thota, S., Karki, S.S., Balzarini, J., De Clercq, E. & Tokuda, H.
    Synthesis of thiocarbohydrazide and carbohydrazide derivatives as possible biologically active agents.
    Med. Chem. Res., 23: 1046-1056 (2014).
    


79. Zhang, L., Zhan, P., Chen, X., Li, Z., Xie, Z., Zhao, T., Liu, H., De Clercq, E., Pannecouque, C., Balzarini, J. & Liu, X.
    Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
    Bioorg. Med. Chem., 22: 633-642 (2014).
    



37 publications in the year 2013



80. De Clercq, E.
    Selective anti-herpesvirus agents.
    Antivir. Chem. Chemother., 23: 93-101 (2013).
    


81. Chen, X., Liu, X., Meng, Q., Wang, D., Liu, H., De Clercq, E., Pannecouque, C., Balzarini, J. & Liu, X.
    Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
    Bioorg. Med. Chem. Lett., 23: 6593-6597 (2013).
    


82. Asundaria, S.T., Pannecouque, C., De Clercq, E., Supuran, C.T. & Patel, K.C.
    Synthesis of novel biologically active methylene derivatives of sydnones.
    Med. Chem. Res., 22: 5752-5763 (2013).
    


83. De Clercq, E.
    Dancing with chemical formulae of antivirals: a panoramic view (part 2).
    Biochem. Pharmacol., 86: 1397-1410 (2013).
    


84. Rai, D., Chen, W., Tian, Y., Chen, X., Zhan, P., De Clercq, E., Pannecouque, C., Balzarini, J. & Liu, X.
    Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
    Bioorg. Med. Chem., 21: 7398-7405 (2013).
    


85. Chen, W., Zhan, P., De Clercq, E., Pannecouque, C., Balzarini, J., Xin Jiang, X. & Liu, X.
    Design, synthesis and biological evaluation of N2, N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.
    Bioorg. Med. Chem., 21: 7091-7100 (2013).
    


86. Wu, H.Q., Yan, Z.H., Chen, W.X., He, Q.-Q., Chen, F.-E., De Clercq, E., Balzarini, J., Daelemans, D. & Pannecouque, C.
    Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: Synthesis, biological investigation and molecular modeling studies.
    Bioorg. Med. Chem., 21: 6477-6483 (2013).
    


87. De Clercq, E.
    The acyclic nucleoside phosphonates (ANPs): Antonín Holý’s legacy.
    Med. Res. Rev., 33: 1278-1303 (2013).
    


88. De Clercq, E.
    A cutting-edge view on the current state of antiviral drug development.
    Med. Res. Rev., 33: 1249-1277 (2013).
    


89. De Clercq, E.
    Highlights in antiviral drug research: antivirals at the horizon.
    Med. Res. Rev., 33: 1215-1248 (2013).
    


90. Thota, S., Vallala, S., Imran, M., Mekala, S., Sunder Anchuri, S., Karki, S.S., Rajeshwar Yerra, R., Balzarini, J. & De Clercq, E.
    Synthesis, spectroscopic characterization, in vitro cytotoxic and structure activity relationships of some mononuclear Ru(II) complexes.
    J. Coord. Chem., 66: 1031-1045 (2013).
    


91. Tian, Y., Rai, D., Zhan, P., Pannecouque, C., Balzarini, J., De Clercq, E., Liu, H. & Liu, X.
    Design, synthesis, and biological evaluation of novel 3,5-disubstituted-1,2,6-thiadiazine-1,1-dione derivatives as HIV-1 NNRTIs.
    Chem Biol Drug Des., 82: 384–393 (2013).
    


92. Li, Z., Cao, Y., Zhan, P., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
    Arylazolylthioacetanilide. Part 11: Design, synthesis and biological evaluation of 1,2,4-triazole thioacetanilide derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
    Med. Chem., 9: 968-973 (2013).
    


93. De Clercq, E.
    Dancing with chemical formulae of antivirals: a personal account.
    Biochem. Pharmacol., 86: 711-725 (2013).
    


94. De Clercq, E.
    The nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors (PIs) in the treatment of HIV infections (AIDS).
    In: “Antiviral Agents”, De Clercq, E., ed. In: Advances in Pharmacology, vol. 67. Enna, S.J., ed. Academic Press, 317-358 (2013).
    


95. De Clercq, E.
    The Holý trinity: the acyclc nucleoside phosphonates.
    In: “Antiviral Agents”, De Clercq, E., ed. In: Advances in Pharmacology, vol. 67. Enna, S.J., ed. Academic Press, 293-316 (2013).
    


96. De Clercq, E.
    Preface
    In: “Antiviral Agents”, De Clercq, E., ed. In: Advances in Pharmacology, vol. 67. Enna, S.J., ed. Academic Press, :ix-xii (2013).
    


97. Chen, X., Li, Y., Ding, S., Balzarini, J., Pannecouque, C., De Clercq, E., Liu, H. Liu, X.
    Discovery of piperidine-linked pyridine analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
    ChemMedChem, 8: 1117-1126 (2013).
    


98. Zhan, P., Chen, X., Li, D., Fang, Z., De Clercq, E. & Liu, X.
    HIV-1 NNRTIs: structural diversity, pharmacophore similarity, and implications for drug design.
    Med. Res. Rev., 33, Suppl. 1: E1-E72 (2013).
    


99. Song, Y., Zhan, P., Kang, D.W., Li, X., Tian, Y., Li, Z.Y., Chen, X.W., Chen, W.M., Pannecouque, C., De Clercq, E. & Liu, X.Y.
    Discovery of novel pyridazinylthioacetamides as potent HIV-1 NNRTIs using a structure-based bioisosterism approach.
    MedChemComm, 4: 810-816 (2013).
    


100. Sunder, A.S., Dhulipala, S., Thota, S., Yerra, R., Balzarini, J. & De Clercq, E.
     Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds.
     J. Res. Med. Sci., 18: 215-221 (2013).
     


101. De Clercq, E.
     Antiviral drug development - success and failure: a personal perspective with a Japanese connection.
     Antivir. Chem. Chemother., 23: 45-55 (2013).
     


102. Yang, S., Pannecouque, C., Daelemans, D., Ma, X.-D., Liu, Y., Chen, F.-E. & De Clercq, E.
     Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 65: 134-143 (2013).
     


103. Kumar, P., Narasimhan, B., Ramasamy, K., Mani, V., Mishra, R.K., Abdul Majeed, A.B. & De Clercq, E.
     N’-[4-[(substituted imino)methyl]benzylidene]-substituted benzohydrazides: synthesis, antimicrobial, antiviral, anticancer evaluation, and QSAR studies.
     Monatsh. Chem. - Chem. Monthly, 144: 825-840 (2013).
     


104. Zoidis, G., Naesens, L. & De Clercq, E.
     An intriguing and facile one-pot catalytic synthesis of N-alkylated lactams.
     Monatsh. Chem. - Chem. Monthly, 144: 515-521 (2013).
     


105. Patel, H.D., Divatia, S.M. & De Clercq, E.
     Synthesis and some novel thiosemicarbazone derivatives having anti-cancer, anti-HIV as well as anti-bacterial activity.
     Ind. J. Chem., 52B: 535-545 (2013).
     


106. Li, W., Zhan, P., De Clercq, E., Lou, H. & Liu, X.
     Current drug research on PEGylation with small molecular agents.
     Progr. Polymer Sci., 38: 421-444 (2013).
     


107. Tsay, S.C., Hwu, J.R., Singha, R., Huang, W.C., Chang, Y.H., Hsu, M.H., Shieh, F.K., Lin, C.C., Hwang, K.C., Horng, J.C., De Clercq, E., Vliegen, I. & Neyts, J.
     Coumarins hinged directly on benzimidazoles and their ribofuranosides to inhibit hepatitis C virus.
     Eur. J .Med. Chem., 63: 290-298 (2013).
     


108. Li, D., Zhan, P., Liu, H., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
     Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
     Bioorg. Med. Chem., 21: 2128-2134 (2013).
     


109. Song, Y., Zhan, P., Li, X., Rai, D., De Clercq, E. & Liu, X.
     Multivalent agents: a novel concept and preliminary practice in anti-HIV drug discovery.
     Curr. Med. Chem., 20: 815-832 (2013).
     


110. Karki, S.S., Kulkarni, A.A., Kumar, S., Kumar Veliyath, S., De Clercq, E. & Balzarini, J.
     Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-N-substituted-hydrazinecarbothioamides.
     Med. Chem. Res., 22: 2014-2022 (2013).
     


111. Patel, N.B., Khan, I.H., Pannecouque, C. & De Clercq, E.
     Anti-HIV, antimycobacterial and antimicrobial studies of newly synthesized 1,2,4-triazole clubbed benzothiazoles.
     Med. Chem. Res., 22: 1320-1329 (2013).
     


112. Tatar, E., Küçükgüzel, I., Daelemans, D., Talele, T.T., Kaushik-Basu, N., De Clercq, E. & Pannecouque, C.
     Some hydrazones of 2-aroylamino-3-methylbutanohydrazide: Synthesis, molecular modeling studies and identification as stereoselective inhibitors of HIV-1.
     Arch. Pharm., 346: 140-153 (2013).
     


113. De Clercq, E.
     Antivirals: past, present and future.
     Biochem. Pharmacol., 85: 727-744 (2013).
     


114. Narang, R., Narasimhan, B., Sharma, S., De Clercq, E., Pannecouque, C. & Balzarini, J
     Substituted naphthalen-1-yl-acetic acid hydrazides: synthesis, antimicrobial evaluation and QSAR analysis.
     Med. Chem., 9: 249-274 (2013).
     


115. Li, Z., Cao, Y., Zhan, P., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
     Synthesis and anti-HIV evaluation of novel 1,2,4-triazole derivatives as potential non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Lett. Drug Design Discov., 10: 27-34 (2013).
     


116. Judge, V., Narasimhan, B., Ahuja, M., Sriram, D., Yogeeswari, P., De Clercq, E., Pannecouque, C. & Balzarini, J.
     Synthesis, antimycobacterial, antiviral, antimicrobial activity and QSAR studies of N-2-acyl isonicotinic acid hydrazide derivatives.
     Med. Chem., 9: 53-76 (2013).
     



38 publications in the year 2012



117. Selvam, P., Lakra, D.R., Pannecouque, C. & De Clercq, E.
     Synthesis, antiviral and cytotoxicity studies of novel N-substituted indophenazine derivatives.
     Indian J. Pharm. Sci., 74: 275–278 (2012).
     


118. Li, X., Zhan, P., De Clercq, E. & Liu, X.
     The HIV-1 non-nucleoside reverse transcriptase inhibitors (Part V): capravirine and its analogues.
     Curr. Med. Chem., 19: 6138-6149 (2012).
     


119. Mahajan, D.H., Chikhalia, K.H., Pannecouque, C. & De Clercq, E.
     Synthesis and anti-HIV evaluation of new 2-thioxoimidazolidin-4-ones and their arylidine (styryl) derivatives.
     Pharm. Chem. J., 46: 165-170 (2012).
     


120. Modh, R.P.,
     Synthesis and evaluation of novel 4-substituted styryl quinazolines as potential antimicrobial agents.
     Arch. Pharm., 345: 964-972 (2012).
     


121. De Clercq, E.
     Organic chemist whose inventions reshaped the antiviral drug world. Editorial.
     Med. Res. Rev., 33: 1-2 (2012).
     


122. De Clercq, E.
     Milestones in the discovery of antiviral agents: nucleosides and nucleotides.
     Acta Pharm. Sinica B, 2: 535-548 (2012).
     


123. Gangarapu, K., Manda, S., Thota, S., Yerra,, R., Karki, S.S., Balzarini, J., De Clercq, E. & Tokuda, H.
     Microwave assisted synthesis, characterization of some new isatin and thiophene derivatives as cytotoxic and chemopreventive agents.
     Lett. Drug Design Discov., 9: 934-941(2012).
     


124. De Clercq, E.
     The race for interferon-freee HCV therapies: a snap shot at early 2012.
     Rev. Med. Virol., 22: 392-411 (2012).
     


125. Zhan, P., Chen, W., Li, Z., Li, X., Chen, X., Tian Y., Pannecouque, C., De Clercq, E. & Liu, X.
     Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
     Biooorg. Med. Chem., 20: 6795-6802 (2012).
     


126. Zhan, P., Li, X., Li, Z., Chen, X., Tian, Y., Chen, W., Liu, X., Pannecouque, C. & De Clercq, E.
     Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
     Bioorg. Med. Chem., 22: 7155-7162 (2012).
     


127. Ahsan, M.J., Govindasamy, J., Khalilullah, H., Mohan, G., Stables, J.P., Pannecouque, C. & De Clercq, E.
     POMA analyses as new efficient bioinformatics' platform to predict and optimise bioactivity of synthesized 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.
     Bioorg Med Chem Lett., 22: 7029-7035 (2012).
     


128. De Clercq, E.
     Human viral diseases: what is next for antiviral drug discovery ?
     Curr. Opin. Virol., 2: 572-579 (2012).
     


129. Tatar, E., Küçükgüzel, I., De Clercq, Krishnan, R. & Kaushit-Basu, N.
     Synthesis, characterization and antiviral evaluation of 1,3-thiazolidine-4-one derivatives bearing L-valine side chain.
     Marmara Pharm. J., 16: 181-193 (2012).
     


130. Li, X., Zhan, P., Liu, H., Li, D., Wang, L., Chen, X., Liu, H., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
     Arylazolyl(azinyl)thioacetanilides. Part 10: Design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
     Bioorg. Med. Chem., 20: 5527-5536 (2012).
     


131. Smith, R., Huskens, D., Daelemans, D., Mewis, R.E., Garcia, C.D., Cain, A.N., Freeman, T.N., Pannecouque, .C, De Clercq, E., Schols, D., Hubin, T.J. & Archibald S.J.
     CXCR4 chemokine receptor antagonists: nickel(II) complexes of configurationally restricted macrocycles.
     Dalton Trans., 41: 11369-11377 (2012).
     


132. Bhattacharya, A.K., Rana, K.C., Pannecouque, C. & De Clercq, E.
     An efficient synthesis of a hydroxyethylamine (HEA) isostere and its α-aminophosphonate and phosphoramidate derivatives as potential anti-HIV agents.
     ChemMedChem, 7: 1601-1611 (2012).
     


133. Zhan, P., Wang, L., Liu, H., Chen, X., Li, X., Jiang, X., Zhang, Q., Liu, X., Pannecouque, C., Naesens, L., De Clercq, E., Liu, A. & Du, G.
     Arylazolyl(azinyl)thioacetanilide. Part 9: Synthesis and biological investigation of thiazolylthioacetamides derivatives as a novel class of potential antiviral agents.
     Arch. Pharm. Res., 35: 975-986 (2012).
     


134. De Clercq, E.
     Tenofovir: quo vadis anno 2012 (where is it going in the year 2012) ?
     Med. Res. Rev., 32: 765-785 (2012).
     


135. Judge, V., Narasimhan, B., Ahuja, M., Sriram, D., Yogeeswari, P., De Clercq, E., Pannecouque, C. & Balzarini, J.
     Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of isonicotinic acid-1-(substituted phenyl)-ethylidene/ cycloheptylidene hydrazides.
     Med. Chem. Res., 21: 1935-1952 (2012).
     


136. Narang, R., Narasimhan, B., Sharma, S., Sriram, D., Yogeeswari, P., De Clercq, E., Pannecouque, C. & Balzarini, J.
     Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of nicotinic acid benzylidene hydrazide derivatives.
     Med. Chem. Res., 21: 1557-1576 (2012).
     


137. Li, Z., Zhan, P., Naesens, L., Vanderlinden, E., Liu, A., Du, G., De Clercq, E. & Liu, X.
     Synthesis and preliminary biologic evaluation of 5-substituted-2-(4-substituted phenyl)-1,3-benzoxazoles as a novel Class of influenza virus A inhibitors.
     Chem. Biol. Drug Des., 79: 1018-1024 (2012).
     


138. Judge, V., Narasimhan, B., Ahuja, M., Sriram, D., Yogeeswari, P., De Clercq, E., Pannecouque, C. & Balzarini, J.
     Isonicotinic acid hydrazide derivatives: synthesis, antimycobacterial activity, and QSAR studies.
     Med. Chem. Res., 21: 1451-1470 (2012).
     


139. Patel, R.V., Kumari, P., Rajani, D.P., Pannecouque, C., De Clercq, E. & Chikhalia, K.H.
     Antimicrobial, anti-TB, anticancer and anti-HIV evaluation of new s-triazine-based heterocycles.
     Future Med. Chem., 4: 1053-1065 (2012).
     


140. De Clercq, E.
     Where rilpivirine meets with tenofovir, the start of a new anti-HIV drug combination era.
     Biochem. Pharmacol., 84: 241-248 (2012).
     


141. Chen, X., Zhan, P., Liu, X., Cheng, Z., Meng, C., Shao, S., Pannecouque, C., De Clercq, E. & Liu, X.
     Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
     Bioorg Med Chem., 20: 3856-3864 (2012).
     


142. Gu, S.-X., Li, Z-.M., Ma, X.-D., Yang, S.-Q., He, Q.-Q., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 53: 229-234 (2012).
     


143. Thota, S., Imran, M., Udugula, M., Karki, S.S., Kanjarla, N., Yerra, R., Balzarini, J. & De Clercq, E.
     Synthesis, spectroscopic characterization, antineoplastic, in vitro-cytotoxic, and antibacterial activities of mononuclear ruthenium(II) complexes.
     J. Coord. Chem., 65: 823-839 (2012).
     


144. Li, D., Zhan, P., De Clercq, E. & Liu, X.
     Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
     J. Med. Chem., 55: 3595-3613 (2012).
     


145. Ross, A., Choi, J.-H., Hunter, T.M., Pannecouque, C., Moggach, S.A., Parsons, S., De Clercq, E. & Sadler, P.J.
     Zinc(II) complexes of constrained antiviral macrocycles.
     Dalton Transactions, 41: 6408-6418 (2012).
     


146. Chen, X., Zhan, P., Pannecouque, C., Balzarini, J., De Clercq, E. & Liu, X.
     Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 51: 60-66 (2012).
     


147. Tian, Y., Zhan, P., Rai, D., Zhang, J., De Clercq, E. & Liu, X.
     Recent advances in the research of 2,3-diaryl-1,3-thiazolidin-4-one derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
     Curr. Med. Chem., 19: 2026-2037 (2012).
     


148. De Clercq, E.
     Ten paths to the discovery of antivirally active nucleoside and nucleotide analogues.
     Nucleosides, Nucleotides & Nucleic Acids, 339-352 (2012).
     


149. Thota, S., Imran, M., Udugula, M., Yerra, R., Karki, S.S., Balzarini, J. & De Clercq, E.
     Synthesis, spectroscopic characterization and in vitro antitumor activities of some novel mononuclear Ru(II) complexes.
     Chin. Chem. Lett., 23: 466-469 (2012).
     


150. Li, W., Wu, J., Zhan, P., Chang, Y., Pannecouque, C., De Clercq, E. & Liu, X.
     Synthesis, drug release and anti-HIV activity of a series of PEGylated zidovudine conjugates.
     Int. J. Biol. Macromol., 50: 974-980 (2012).
     


151. Yang, S., Chen, F.-E. & De Clercq, E.
     Dihydro-alkoxyl-benzyl-oxopyrimidine derivatives (DABOs) as non-nucleoside reverse transcriptase inhibitors: an update review (2001-2011)
     Curr. Med. Chem., 19: 152-162 (2012).
     


152. Chen, W., Zhan, P., De Clercq, E. & Liu, X.
     Recent progress in small molecule CCR5 antagonists as potential HIV-1 entry inhibitors.
     Curr. Pharm. Des., 18: 100-112 (2012).
     


153. Mironiuk-Puchalska, E., Koszytkowska-Stawińska, M., Sas, W., De Clercq, E. & Naesens, L.
     Synthesis of novel AZA-analogues of tiazofurin with 2-[5,5-bis(hydroxymethyl)-pyrrolidin-2-yl] framework as sugar mimic.
     Nucleosides Nucleotides Nucleic Acids, 31: 72-84 (2012).
     


154. De Clercq, E.
     Pre-exposure chemoprophylaxis of HIV infection: Quo vadis ?
     Biochem. Pharmacol., 83: 567-573 (2012).
     



39 publications in the year 2011



155. Zhan, P., Yan, R.Z., Liu, X.Y., Pannecouque, C., Witvrouw, M., De Clercq, E., Molina, M.T. & Vega, S.
     Synthesis and anti-HIV activity of novel 2,4-disubstituted-7-methyl-1,1,3-trioxo-2H,4H-pyrazolo[4,5-e][1,2,4]thiadiazine derivatives.
     Drug Discov. Ther., 5: 279-285 (2011).
     


156. Karki, S.S., Thota, S., Katiyar, A., Jayaveera, K.N., De Clercq, E. & Balzarini, J.
     Synthesis, characterization and cytotoxic activity of some Ru(II) complexes.
     Turk. J. Chem., 8: 207-218 (2011).
     


157. Ma, X.D., Yang, S.Q., Gu, S.X., He, Q.Q., Chen, F.E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and anti-HIV activity of aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as potent non-nucleoside reverse transcriptase Iinhibitors.
     ChemMedChem, 6: 2225-2232 (2011).
     


158. Kulik, K., Radzikowska, E., Kaczmarek, R., Baraniak, J., Stec, W.J., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and an antiviral activity evaluation of nucleoside 5’-O-(N-acyl) phosphoramidates.
     Antiviral Chem. Chemother., 21: 143-150 (2011).
     


159. Gu, S.-X., Yang, S.-Q., He, Q.-Q., Ma, X.-D., Chen, F.-E., Dai, H.-F., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
     Bioorg. Med. Chem., 19: 7093-7099 (2011).
     


160. Karki, S.S., Bhutle, S.R., Sahoo, S., Reddy, R., Balzarini, J., De Clercq, E. & Darji, S.Y.
     Synthesis and biological evaluation of some stilbene derivatives.
     Med. Chem. Res., 20: 1349-1356 (2011).
     


161. Karki, S.S., Kulkarni, A., Teraiya, N., De Clercq, E. & Balzarini, J.
     Synthesis and cytostatic evaluation of some 2-(5-substituted-2-oxoindolin-3-ylidene)-N-substituted hydrazine carbothioamide.
     Med. Chem. Res., 20: 1229-1234 (2011).
     


162. Das, S., Das, U., Varela-Ramírez, A., Lema, C., Aguilera, R.J., Balzarini, J., De Clercq, E., Dimmock, S.G., Gorecki, D.K. & Dimmock J.R.
     Bis[3,5-bis(benzylidene)-4-oxo-1-piperidinyl]amides: a novel class of potent cytotoxins.
     ChemMedChem, 6: 1892-1899 (2011).
     


163. Zhan, P., Chen, X., Li, X., Li, D., Tian, Y., Chen, W., Pannecouque, C., De Clercq, E. & Liu, X.
     Arylazolylthioacetanilide. Part 8☆: Design, synthesis and biological evaluation of Novel 2-(2-(2,4-Dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides As Potent HIV-1 inhibitors.
     Eur. J. Med. Chem., 46, 5039-5045 (2011).
     


164. De Clercq, E.
     HIV life cycle: targets for anti-HIV agents.
     In: HIV-1 Integrase: Mechanism and Inhibitor Design”, N. Neamati (ed.). Wiley Series in Drug Discovery and Development, B. Wang (series ed.), Wiley-VCH, Weinheim, Germany, pp. 1-14 (2011).
     


165. Yu, M., Liu, A., Du, G., Naesens, L., Vanderlinden, E., De Clercq, E. & Liu, X.
     Discovery of dihydro-alkyloxy-benzyl-oxopyrimidines as promising anti-influenza virus agents.
     Chem. Biol. Drug Des., 78: 596-602 (2011).
     


166. De Clercq, E.
     Antiviral Research, at its 30th anniversary, remembrances from its Editor-in-Chief. Editorial.
     Antiviral Res., 92: 1-6 (2011).
     


167. De Clercq, E.
     Discovery and development of tenofovir disoproxil fumarate.
     In: “Antiviral Drugs. From Basic Discovery through Clinical Trials”, W.M. Kazmierski (ed.). John Wiley & Sons, Inc., Hoboken, NJ, USA, pp. 85-101 (2011).
     


168. Selvam, P., Chandramohan, M., Pannecouque, C. & De Clercq, E.
     Studies on antiviral activity of 2,3-diphenylquinoxaline.
     Int. J. Pharm. & Ind. Res., 1: 138-140 (2011).
     


169. Gu, S.-X., He, Q.-Q., Yang, S.-Q., Ma, X.-D., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and structure–activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
     Bioorg. Med. Chem., 19: 5117-5124 (2011).
     


170. Završnik, D., Muratović, S., Makuc, D., Plavec, J., Cetina, M., Nagl, A., De Clercq, E., Balzarini, J. & Mintas, M.
     Benzylidene-bis-(4-hydroxycoumarin) and benzopyranocoumarin derivatives: synthesis, 1H/13C NMR conformational and X-ray crystal structure studies and in vitro antiviral activity evaluations.
     Molecules, 16: 6023-6040 (2011).
     


171. Yu, M., Li, Z., Liu, S., Fan, E., Pannecouque, C., De Clercq, E. & Liu, X.
     Synthesis and biological evaluation of 6-substituted 5-alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs.
     ChemMedChem, 6: 826-833 (2011).
     


172. Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3, 4-dihydroquinolin-1(2H)-yl) methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Zhang, J., Zhan, P., Wu, J., Li, Z., Jiang, Y., Ge, W., Pannecouque, C., De Clercq, E. & Liu, X.
     Bioorg. Med. Chem., 19: 4366-4376 (2011).
     


173. De Clercq, E.
     Acyclic nucleoside phosphonates: an unfinished story.
     Collect. Czech. Chem. Commun., 76: 829-842 (2011).
     


174. Ali, M.A., Ismail, R., Choon, T.S., Yoon, Y.K., Wei, A.C., Pandian, S., Samy, J.G., De Clercq, E. & Pannecouque, C.
     Synthesis and anti-HIV activity of novel 3-substituted phenyl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]isoxazole analogues.
     Acta Pol. Pharm., 68, 343-348 (2011).
     


175. Zhang, J., Ge, W., Zhan, P., De Clercq, E. & Liu, X.
     Retroviral restriction factors TRIM5α: therapeutic strategy to inhibit HIV-1 replication.
     Curr. Med. Chem., 18: 2649-2654 (2011).
     


176. Daelemans, D., Pauwels, R., De Clercq, E. & Pannecouque, C.
     A time-of-drug-addition approach to target identification of antiviral compounds.
     Nat. Protocol., 6: 925-933 (2011).
     


177. De Clercq, E.
     The clinical potential of the acyclic (and cyclic) nucleoside phosphonates. The magic of the phosphonate bond.
     Biochem. Pharmacol., 82: 99-109 (2011).
     


178. Das, U., Pati, H.N., Sakagami, H., Hashimoto, K., Kawase, M., Balzarini, J., De Clercq, E. & Dimmock, J.R.
     3,5-bis(Benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]-piperidin-4-ones: A novel cluster of potent tumor-selective cytotoxins.
     J. Med. Chem., 54: 3445-3449 (2011).
     


179. Kumar, S.S., Kumar, Y., Khan, M.S.Y., Anbu, J. & De Clercq, E.
     Antihistaminic and antiviral activities of steroids of Turbinaria conoides.
     Nat. Prod. Res., 25: 723-729 (2011).
     


180. Hwu, J.R., Lin, S.Y., Tsay, S.C., De Clercq, E., Leyssen, P. & Neyts, J.
     Coumarin-purine ribofuranoside conjugates as new agents against hepatitis C virus.
     J. Med. Chem., 54: 2114-2126 (2011).
     


181. Baszczyňski, O., Jansa, P., Dračínský, M., Klepetářová, B., Holý, A., Votruba, I., Balzarini, J., De Clercq, E. & and Janeba, Z.
     Synthesis and antiviral activity of N9-[3-fluoro-2-(phosphonomethoxy)propyl] analogues derived from N6-substituted adenines and 2,6-diaminopurines.
     Bioorg. Med. Chem., 19: 2114-2124 (2011).
     


182. Skerlj, R., Bridger, G., McEachern, E., Harwig, C., Smith, C., Kaller, A., Veale, D., Yee, H., Skupinska, K., Wauthy, R., Wang, L., Baird, I., Zhu, Y., Burrage, K., Yang, W., Sartori, M., Huskens, D., De Clercq, E. & Schols, D.
     Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
     Bioorg. Med. Chem. Lett., 21: 1414-1418 (2011).
     


183. Desai, S.D., Desai, K.R., Chikhalia, K.H., Pannecouque, C. & De Clercq, E.
     Synthesis of a novel class of some 1,3,5-triazine derivatives and their anti-HIV activity.
     Int. J. Drug Des. Discov., 2: 361-368 (2011).
     


184. Chen, X., Zhan, P., Li, D., De Clercq, E. & Liu, X.
     Recent advances in DAPYs and related analogues as HIV-1 NNRTIs.
     Curr. Med. Chem., 18: 359-376 (2011).
     


185. Zhan, P., Li, D., Chen, X., Liu, X. & De Clercq, E.
     Functional roles of azole motif in anti-HIV agents.
     Curr. Med. Chem., 18: 29-46 (2011).
     


186. Jiang, Y., Liu, X. & De Clercq, E.
     New therapeutic approaches targeted at the late stages of the HIV-1 replication cycle.
     Curr. Med. Chem., 18: 16-28 (2011).
     


187. Somani, R.R., Agrawal, A.G., Bhanushali, U.V., Kalantri, P.P. & De Clercq, E.
     Synthesis and biologica evaluation of some 2,5-disubstituted-1,3,4-oxadiazole derivatives.
     Int. J. Drug Design Discov., 2: 413-418 (2011).
     


188. Somani, R.R., Agrawal, A.G., Kalantri, P.P., Gavarkat, P.S. & De Clercq, E.
     Investigation of 1,3,4-oxadiazole scaffold as potentially active compounds.
     Int. J. Drug Design Discov., 2: 353-360 (2011).
     


189. De Clercq, E.
     A 40-year journey in search of selective antiviral chemotherapy.
     Annu. Rev. Pharmacol. Toxicol., 51: 1-24 (2011).
     


190. De Clercq, E.
     From TIBO to rilpivirine: the chronicle of the discovery of the ideal nonnucleoside reverse transcriptase inhibitor.
     In: “Antiviral Drug Strategies”, E. De Clercq (ed.). “Methods and Principles in Medicinal Chemistry”, R. Mannhold, H. Kubinyi & G. Folkers (eds.). Wiley-VCH Verlag GmbH & Co., Weinheim, Germany, pp. 377-389 (2011).
     


191. De Clercq, E.
     Outlook of the antiviral drug era, now more than 50 years after description of the first antiviral drug.
     In: “Antiviral Drug Strategies”, E. De Clercq (ed.). “Methods and Principles in Medicinal Chemistry”, R. Mannhold, H. Kubinyi & G. Folkers (eds.). Wiley-VCH Verlag GmbH & Co., Weinheim, Germany, pp. 1-28 (2011).
     


192. Skerlj, R., Bridger, G., McEachern, E., Harwig, C., Smith, C., Wilson, T., Veale, D., Yee, H., Crawford, J., Skupinska, K., Wauthy, R., Yang, W., Zhu, Y., Bogucki, D., Di Fluri, M., Langille, J., Huskens, D., De Clercq, E. & Schols, D.
     Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
     Bioorg. Med. Chem. Lett., 21: 262-266 (2011).
     


193. De Clercq, E.
     The next ten stories on antiviral drug discovery (part E): advents, advances and adventures.
     Med. Res. Rev., 31: 118-160 (2011).
     



51 publications in the year 2010



194. Selvam, P., Pannecouque, C. & De Clercq, E.
     Synthesis and antiviral activity of some novel 6-bromo/6,8-dibromo, N-benzoyl-4-(4-oxo-2-phenyl-4H-quinazolin-3-yl)-benzenesulphonamide.
     Int. J. Chem. Sci., 8: 716-720 (2010).
     


195. Selvam, P., Murugesh, N., Chandramohan, M., Pannecouque, C. & De Clercq, E.
     Synthesis, antiviral and cytotoxic activities of 2-(2-phenyl carboxylic acid)-3-phenylquinazolin-4(3H)-ones.
     Indian J. Pharm. Sci., 72: 806-809 (2010).
     


196. Yadav, S., Kumar, P., De Clercq, E., Balzarini, J., Pannecouque, C., Dewan, S.K. & Narasimhan, B.
     4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: Synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
     Eur. J. Med. Chem., 45: 5985-5997 (2010).
     


197. Li, W., Chang, Y., Zhan, P., Zhang, N., Liu, X., Pannecouque, C. & De Clercq, E.
     Synthesis, in vitro and in vivo release kinetics, and anti-HIV activity of a sustained-release prodrug (mPEG-AZT) of 3’-azido-3’-deoxythymidine (AZT, zidovudine).
     ChemMedChem, 5: 1893-1898 (2010).
     


198. De Clercq, E.
     Prospects of anti-HIV therapy.
     Proceedings of the Centennial Retrovirus Meeting (CRM), Institute of Molecular Genetics, Prague, Czech Republic, 29 April-4 May 2010. Daniek, R., Hejnar, J., Skalka, A.M. & Svoboda, J., eds. Medimond, Bologna, Italy, pp. 61-66 (2010).
     


199. De Clercq, E.
     Recent advances on the use of the CXCR4 antagonist plerixafor (AMD3100, MozobilTM) and potential of other CXCR4 antagonists as stem cell mobilizers.
     Pharmacol. Ther., 128: 509-518 (2010).
     


200. Krečmerová, M., Holý, A., Andrei, G., Pomeisl, K., Tichý, T., Břehová, P., Masojídková, M., Dračínský, M., Pohl, R., Laflamme, G., Naesens, L., Hui, H., Cihlar, T., Neyts, J., De Clercq, E., Balzarini, J. & Snoeck, R.
     Synthesis of ester prodrugs of 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents.
     J. Med. Chem., 53: 6825-6837 (2010).
     


201. Kumar, K.S., Ganguly, S., Veerasamy, R. & De Clercq, E.
     Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
     Eur. J. Med. Chem., 45: 5474-5479 (2010).
     


202. Zoidis, G., Kolocouris, N., Kelly, J.M. Prathalingam, S.R., Naesens, L. & De Clercq, E.
     Design and synthesis of bioactive adamantanaminoalcohols and adamantanamines.
     Eur. J. Med. Chem., 45: 5022-5030 (2010).
     


203. Holý, A. & De Clercq, E.
     Anti-DNA virus agents.
     In: Burger’s Medicinal Chemistry, Drug Discovery and Development”, 7th ed. Abraham, D.J. & Rotella, D.P., eds. John Wiley & Sons, Inc., Hoboken, NJ, USA, pp. 221-258 (2010).
     


204. De Clercq, E.
     HIV reverse transcriptase inhibitors.
     In: Burger’s Medicinal Chemistry, Drug Discovery and Development”, 7th ed. Abraham, D.J. & Rotella, D.P., eds. John Wiley & Sons, Inc., Hoboken, NJ, USA, pp. 139-168 (2010).
     


205. De Clercq, E.
     Antiretroviral drugs.
     Curr. Opin. Pharmacol., 10: 507-515 (2010).
     


206. De Clercq, E.
     The paths to the discovery of antivirally active nucleoside and nucleotide analogues.
     Proceedings of the IRT 2010 - XIX International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Lyon, France, 29th August-3rd September 2010.
     http://irt2010.univ-lyon1.fr (2010).
     


207. Benci, K., Wittine, K., Radan, M., Cetina, M., Sedić, M., Kraljević Pavelić, S.K., Pavelić, K., De Clercq, E. & Mintas, M.
     The unsaturated acyclic nucleoside analogues bearing a sterically constrained (Z)-4’-benzamido-2’-butenyl moiety: synthesis, X-ray crystal structure study, cytostatic and antiviral activity evaluation.
     Bioorg. Med. Chem., 18: 6249-6257 (2010).
     


208. Singh, R.K., Yadav, D., Rai, D., Kumari, G., Pannecouque, C. & De Clercq, E.
     Synthesis, structure–activity relationship and antiviral activity of 3′-N,N-dimethylamino-2′,3′-dideoxythymidine and its prodrugs.
     Eur. J. Med. Chem., 45: 3787-3793 (2010).
     


209. Zhan, P., Liu, H., Liu, X., Wang, Y., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and anti-HIV activity evaluation of novel N’-arylidene-2-[1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio)acetohydrazides.
     Med. Chem. Res., 19: 652-663 (2010).
     


210. Thomson, P.F., Lagisetty, P., Balzarini, J., De Clercq, E. & Lakshman, M.K.
     Palladium-catalyzed aryl amination reactions of 6-bromo- and 6-chloropurine nucleosides.
     Adv. Synth. Catal., 352: 1728-1735 (2010).
     


211. Zhan, P., Liu, X.-Y., Li, Z.-Y., Fang, Z.-J., Pannecouque, C. & De Clercq, E.
     Synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-y]sulfanyl}acetamides as HIV-1 inhibitors.
     Chem. Biodiversity, 7: 1717-1727 (2010).
     


212. Zhang, X., Qu, Y., Fan, X., Bores, C., Feng, D., Andrei, G., Snoeck, R., De Clercq, E. & Loiseau, P.M.
     Solvent-free synthesis of pyrimidine nucleoside-aminophosphonate hybrids and their biological activity evaluation.
     Nucleosides, Nucleotides and Nucleic Acids, 29: 516-627 (2010).
     


213. De Clercq, E.
     Antiviral therapy: quo vadis ? (Editorial).
     Future Med. Chem., 2: 1049-1053 (2010).
     


214. Zeng, Z.-S., He, Q.-Q., Liang, Y.-H., Feng, X.-Q., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved HIV-1 chemotherapy.
     Bioorg. Med. Chem., 18: 5039-5047 (2010).
     


215. Thota, S., Karki, S.S., Jayaveera, K.N., Balzarini, J., De Clercq, E.
     Synthesis, antineoplastic and cytotoxic activities of some mononuclear Ru(II) complexes.
     J. Enzyme Inhib. Med. Chem., 25: 513-519 (2010).
     


216. Marchal, A., Nogueras, M., Sánchez, A., Low, J.N., Naesens, L., De Clercq, E. & Melguizo, M.
     Alkoxy-5-nitrosopyrimidines: useful building block for the generation of biologically active compounds.
     Eur. J. Org. Chem., 2010: 3823-3830 (2010).
     


217. Lannang, A.M., Louh, G.N., Biloa, B.M., Komguem, J., Mbazoa, C.D., Sodengam, B.L., Naesens, L., Pannecouque, C., De Clercq, E. & El Ashry, E.S.H.
     Cytotoxicity of natural compounds isolated from the seed of Garcinia afzelii.
     Planta Medica, 76: 708-712 (2010).
     


218. Janeba, Z., Holý, A., Pohl, R., Snoeck, R., Andrei, G., De Clercq, E. & Balzarini, J.
     Synthesis and biological evaluation of acyclic nucleotide analogues with a furo [2,3-d]pyrimidin-2(3H)-one base.
     Can. J. Chem., 88: 628-638 (2010).
     


219. Charlier, N., Davidson, A., Dallmeier, K., Molenkamp, R., De Clercq, E. & Neyts, J.
     Replication of not-known-vector flaviviruses in mosquito cells is restricted by intracellular host factors rather than by the viral envelope proteins.
     J. Gen. Virol., 91: 1693-1697 (2010).
     


220. Liang, Y.-H., He, Q.-Q., Zeng, Z.-S., Liu, X.-Q., Feng, X.-Q., Chen, F.-E., Balzarini, J., Pannecouque, C. & De Clercq, E.
     Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors..
     Bioorg. Med. Chem., 18: 4601-4605 (2010).
     


221. De Clercq, E.
     Historical perspectives in the development of antiviral agents against poxviruses.
     Viruses, 2: 1322-1339 (2010).
     


222. De Clercq, E., Férir, G., Kaptein, S. & Neyts, J.
     Antiviral treatment of chronic hepatitis B virus (HBV) infections.
     Viruses, 2: 1279-1305 (2010).
     


223. Zeng, Z.-S., Liang, Y.-H., Feng, X.-Q., Chen, F.-E., Pannecouque, C., Balzarini, J. & De Clercq, E.
     Lead optimization of diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptases.
     ChemMedChem, 5: 837-840 (2010).
     


224. Kumar, D., Judge, V., Narang, R., Sangwan, S., De Clercq, E., Balzarini, J. & Narasimhan, B.
     Benzylidene/2-chlorobenzylidene hydrazides: synthesis, antimicrobial activity, QSAR studies and antiviral evaluation.
     Eur. J. Med. Chem., 45: 2806-2816 (2010).
     


225. De Clercq, E.
     Yet another ten stories on antiviral drug discovery (part D): paradigms, paradoxes and paraductions.
     Med. Res. Rev., 30: 667-707 (2010).
     


226. Asaftei, S. & De Clercq, E.
     “Viologen” dendrimers as antiviral agents. The effect of charge number and distance.
     J. Med. Chem., 53: 3480-3488 (2010).
     


227. Skerlj, R.T., Bridger, G.J., Kaller, A., McEachern, E.J., Crawford, J.B., Zhou, Y., Atsma, B., Langille, J., Nan, S., Veale, D., Wilson, T., Harwig, C., Hatse, S., Princen, K., De Clercq, E. & Schols, D.
     Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
     J. Med. Chem., 53: 3376-3388 (2010).
     


228. Chen, H., Liu, X., Zhan, P. & De Clercq, E.
     TSG101: a novel anti-HIV-1 drug target.
     Curr. Med. Chem., 17: 750-758 (2010).
     


229. Zhan, P., Liu, X. & De Clercq, E.
     Blocking nuclear import of pre-integration complex: an emerging ant-HIV-1 drug discovery paradigm.
     Curr. Med. Chem., 17: 495-503 (2010).
     


230. De Clercq, E.
     Strategies for the treatment of dengue virus infections: a narrative account.
     Future Med. Chem., 2: 601-608 (2010).
     


231. Feng, X.-Q., Zeng, Z.-S., Liang, Y.-H., Chen, F.-E., Pannecouque, C., Balzarini, J. & De Clercq, E.
     Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
     Bioorg. Med. Chem., 18: 2370-2374 (2010).
     


232. Jha, A., Mukherjee, C., Prasad, A.K., Parmar, V.S., Vadaparti, M., Das, U., De Clercq, E., Balzarini, J., Stables, J.P., Shrivastav, A., Sharma, R.K. & Dimmock, J.R.
     Derivatives of aryl amines containing the cytotoxic 1,4-dioxo-2-butenyl pharmacophore.
     Bioorg. Med. Chem. Lett., 20: 1510-1515 (2010).
     


233. De Clercq, E.
     Highlights in the discovery of antiviral drugs: a personal retrospective
     J. Med. Chem., 53: 1438-1450 (2010).
     


234. Singh, R.K., Rai, D., Yadav, D., Bhargava, A., Balzarini, J. & De Clercq, E.
     Synthesis, antibacterial and antiviral properties of curcumin bioconjugates bearing dipeptide, fatty acids and folic acid.
     Eur. J. Med. Chem., 45: 1078-1086 (2010).
     


235. Monforte, A.-M., Logoteta, P., De Luca, L., Iraci, N., Ferro, S., Maga, G., De Clercq, E., Pannecouque, C. & Chimirri, A.
     Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Bioorg. Med. Chem., 18: 1702-1710 (2010).
     


236. Fan, X., Feng, D., Qu, Y., Zhang, X., Wang, J., Loiseau, P.M., Andrei, G., Snoeck, R. & De Clercq, E.
     Practical and efficient synthesis of pyrano[3,2-c]pyridone, pyrano[4,3-b]pyran and their hybrids with nucleoside as potential antiviral and antileishmanial agents.
     Bioorg. Med. Chem. Lett., 20: 809-813 (2010).
     


237. Bridger, G.J., Skerlj, R.T., Hernandez-Abad, P.E., Bogucki, D.E., Wang, Z., Zhou,Y., Nan, S., Boehringer, E.M., Wilson, T., Crawford, J., Metz, M., Hatse, S., Princen, K., De Clercq, E. & Schols, D.
     Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: Analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication.
     J. Med. Chem., 53: 1250-1260 (2010).
     


238. Daelemans, D., Dumont, J.-M., Rosenwirth, B., De Clercq, E. & Pannecouque, C.
     Debio-025 inhibits HIV-1 by interfering with an early event in the replication cycle.
     Antiviral Res., 85: 418-421 (2010).
     


239. Mehellou, Y. & De Clercq, E.
     Twenty-six years of anti-HIV drug discovery : where do we stand and where do we go ?
     J. Med. Chem., 53: 521-538 (2010).
     


240. Martin, J.C., Hitchcock, M.J.M., De Clercq, E. & Prusoff, W.H.
     Early nucleoside reverse transcriptase inhibitors for the treatment of HIV: A brief history of stavudine (D4T) and its comparison with other dideoxynucleosides.
     Antiviral Res., 85: 34-38 (2010).
     


241. De Clercq, E.
     In search of a selective therapy of viral infections.
     Antiviral Res., 85: 19-24 (2010).
     


242. Cikla, P., Küçükgüzel, S.G., Küçükgüzel, I., Rollas, S., De Clercq, E., Pannecouque, C., Andrei, G., Snoeck, R., Sahin, F. & Bayrak, Ö.F.
     Synthesis and evaluation of antiviral, antitubercular and anticancer activities of some novel thioureas derived from 4-aminobenzohydrazide hydrazones.
     Marmara Pharm. J., 14: 13-20 (2010).
     


243. Tatar, E., Küçükgüzel, I., Küçükgüzel, Ş.G., Yilmaz-Demircan, F., De Clercq, E., Andrei, G., Snoeck, R., Pannecouque, C., Şahin, F. & Bayrak, O.F.
     Synthesis, anti-tuberculosis and antiviral activity of novel 2-isonicotinoylhydrazono-5-arylidene-4-thiazolidinones.
     Int. J. Drug Design Discov., 1: 19-32 (2010).
     


244. Ross, A., Soares, D.C., Covelli, D., Pannecouque, C., Budd, L., Collins, A., Robertson, N., Parsons, S. De Clercq, E., Kennepohl, P. & Sadler, P.J.
     Oxovanadium(IV) cyclam and bicyclam complexes: potential CXCR4 receptor antagonists.
     Inorg. Chem., 49: 1122-1132 (2010).
     



62 publications in the year 2009



245. De Clercq, E.
     Antiviral chemotherapy anno 2009: quo vadis ?
     Future Virol., 4: 313-315 (2009).
     


246. De Clercq, E.
     A new drug combination therapy for treatment-naïve patients with HIV-1 infection, consisting of raltegravir, emtricitabine and tenofovir disoproxil fumarate (TDF).
     Exp. Opin. Pharmacother., 10: 2935-2937 (2009).
     


247. Zhan, P., Liu, X., Pannecouque, C. & De Clercq, E.
     Design strategies of novel NNRTIs to overcome drug resistance.
     Curr. Med. Chem., 16: 3903-3917 (2009).
     


248. Karki, S.S., Hazare, R., Kumar, S., Bahaduria, V.S., Balzarini, J. & De Clercq, E.
     Synthesis, anticancer and cytostatic activity of some 6H-indolo[2,3-b]quinoxalines.
     Acta Pharm., 59: 431-440 (2009).
     


249. De Clercq, E.
     Antiviral drugs.
     In: “Textbook of Drug Design and Discovery”, 4th ed., P. Krogsgaard-Larsen, K. Strømgaard & U. Madsen (eds.). CRC Press, Boca Raton, FL, USA, pp. 393-417 (2009).
     


250. Yu, M., Liu, X., Li, Z., Liu, S., Pannecouque, C. & De Clercq, E.
     Synthesis and biological evaluation of novel 2-(substituted phenylaminocarbonylmethyl-thio)-6-(2,6-dichlorobenzyl)-pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs.
     Biooorg. Med. Chem., 17: 7749-7754 (2009).
     


251. Das, S., Das, U., Selvakumar, P., Sharma, R.K., Balzarini, J., De Clercq, E., Molnár, J., Serly, J., Baráth, Z., Schatte, G., Bandy, B., Gorecki, D.K.J. & Dimmock, J.R.
     3,5-bis(Benzylidene)-4-oxo-1-phosphonopiperidines and related diethyl esters: potent cytotoxins with multi-drug-resistance reverting properties.
     ChemMedChem, 4: 1831-1840 (2009).
     


252. Zhan, P., Liu, X., Fang, Z., Li, Z., Pannecouque, C. & De Clercq, E.
     Synthesis and anti-HIV activity evaluation of 2-(4-naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 44: 4648-4653 (2009).
     


253. Youssef, D., Potter, E., Jha, M., De Clercq, E., Balzarini, J., Stables, J.P. & Jha, A.
     Design, synthesis and bioevaluation of novel maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones as cytostatic agents.
     Bioorg. Med. Chem. Lett., 19: 6364-6367 (2009).
     


254. Cullen, M.D., Ho, W.C., Bauman, J.D., Das, K., Arnold, E., Hartman, T.L., Watson, K.M., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E. Cushman, M.
     Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
     J. Med. Chem., 52: 6467-6473 (2009).
     


255. Tušek-Božić, L., Pannecouque, C., De Clercq, E. & Balzarini, J.
     Sodium and potassium benzeneazophosphonate complexes with crown ethers: solid-state microwave synthesis, characterization and biological activity.
     Polyhedron, 28: 3449-3458 (2009).
     


256. Sharma, D., Narasimhan, B., Kumar, P., Judge, V., Narang, R., De Clercq, E. & Balzarini, J.
     Synthesis, antimicrobial and antiviral activity of substituted benzimidazoles.
     J. Enzyme Inhib. Med. Chem., 24: 1161-1168 (2009).
     


257. Andrei, G., De Clercq, E. & Snoeck, R.
     Viral DNA polymerase inhibitors.
     In: Viral Genome Replication. Götte, M., Cameron, C.E. & Raney, K.D. (eds.). Springer Verlag, pp. 481-526 (2009).
     


258. De Clercq, E.
     Interferon: the quintessence of a quinquagenarian.
     Verh. K. Acad. Geneesk. Belg., 71: 5-14 (2009).
     


259. De Clercq, E.
     The history of antiretrovirals: key discoveries over the past 25 years.
     Rev. Med. Virol., 19; 287-299 (2009).
     


260. Liang, Y.-H., Feng, X.-Q., Zeng, Z.-S., Chen, F.-E., Balzarini, J., Pannecouque, C. & De Clercq, E.
     Design, synthesis, and SAR of naphthyl-substituted diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
     ChemMedChem, 4: 1537-1545 (2009).
     


261. De Clercq, E.
     Anti-HIV drugs: twenty-five compounds approved within twenty-five years after the discovery of HIV.
     Proceedings of the International Conference on Drug Design and Discovery for Developing Countries, Trieste, Italy, 3-5 July 2008.
     In: Drug Design and Discovery for Developing Countries. Megnassan, E., Owono Owono, L. & Miertus, S., eds. ICS-UNID0, Trieste, Italy, pp. 5-39 (2009).
     


262. Zhan, P., Liu, X., Fang, Z., Pannecouque, C. & De Clercq, E.
     1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation.
     Bioorg. Med. Chem., 17: 6374-6379 (2009).
     


263. De Clercq, E.
     Looking back in 2009 at the dawning of antiviral therapy now 50 years ago: an historical perspective.
     Adv. Virus Res., 73: 1-53 (2009).
     


264. Monforte, A.-M., Logoteta, P., Ferro, S., De Luca, L., Iraci, N., Maga, G., De Clercq, E., Pannecouque, C. & Chimirri, A.
     Design, synthesis and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
     Bioorg. Med. Chem., 17: 5962-5967 (2009).
     


265. Zhan, P., Liu, X., Li, Z., Fang, Z., Li, Z., Wang, D., Pannecouque, C. & De Clercq, E.
     Novel 1,2,3-thiadiazole derivatives as HIV-1 NNRTIs with improved potency: synthesis and preliminary SAR studies.
     Bioorg. Med. Chem., 17: 5920-5927 (2009).
     


266. Zhan, P., Liu, X., Zhu, J., Fang, Z., Li, Z., Pannecouque, C. & De Clercq, E.
     Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Bioorg. Med. Chem., 17: 5775-5781 (2009).
     


267. Januszczyk, P., Fogt, J., Boryski, J., Izawa, K., Onishi, T., Neyts, J. & De Clercq, E.
     Synthesis and antiviral evaluation of 2’-C-methyl analogues of 5-alkynyl- and 6-alkylfurano- and pyrrolo[2,3-d]pyrimidine ribonucleosides.
     Nucleosides, Nucleotides & Nucleic Acids, 28: 713-723 (2009).
     


268. De Clercq, E.
     The unabated synthesis of new nucleoside analogues with antiviral potential: a tribute to Morris J. Robins.
     Nucleosides, Nucleotides & Nucleic Acids, 28: 586-600 (2009).
     


269. Shahar Yar, M., Abdullah, M.M., Husain, A., Bakht, M.A. & De Clercq, E.
     Synthesis and evaluation of in vitro antiviral activity of 2-[3-(substituted phenyl)-4,5-dihydro-1H-5-pyrazolyl]benzofuran-3-yl chloride derivatives.
     J. Enzyme Inhib. Med. Chem., 24: 949-956 (2009).
     


270. Karakuş, S., Küçükgüzel, S.G., Küçükgüzel, I., De Clercq, E., Pannecouque, C., Andrei, G., Snoeck, R., Şahin, F. & Bayrak, Ö.F.
     Synthesis, antiviral and anticancer activity of some novel thioureas derived from N-(4-nitro-2-phenoxyphenyl)-methanesulfonamide.
     Eur. J. Med. Chem., 44: 3591-3595 (2009).
     


271. Zhan, P., Li, Z., Liu, X. & De Clercq, E.
     Sulfanyltriazole/tetrazoles: a promising class of HIV-1 NNRTIs.
     Mini-Rev. Med. Chem., 9: 1014-1023 (2009).
     


272. Feng, X.-Q., Liang, Y.-H., Zeng, Z.-S., Chen, F.-E., Balzarini, J., Pannecouque, C. & De Clercq, E.
     Structural modifications of DAPY analogues with potent anti-HIV-1 activity.
     ChemMedChem, 4: 219-224 (2009).
     


273. Mahajan, D.H., Pannecouque, C., De Clercq, E. & Chikhalia, K.H.
     Synthesis and studies of new 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives as potential anti-HIV agents.
     Arch. Pharm. Chem. Life Sci., 342: 281-290 (2009).
     


274. Ostrowski, T., Golankiewicz, B., De Clercq, E., Andrei, G. & Snoeck, R.
     Synthesis and anti-VZV activity of 6-heteroaryl derivatives of tricyclic acyclovir and 9-{[cis-1’,2’-bis(hydroxymethyl)cycloprop-1’-yl]methyl}guanine analogues.
     Eur. J. Med. Chem., 44: 3313-3317 (2009).
     


275. Das, U., Pati, H.N., Panda, A.K., De Clercq, E., Balzarini, J., Molnár, J., Baráth, Z., Ocsovszki, I., Kawase, M., Zhou, L., Sakagami, H. & Dimmock, J.R.
     2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides: a novel cluster of tumor-specific cytotoxins which reverse multidrug resistance.
     Bioorg. Med. Chem., 17: 3909-3915 (2009).
     


276. Koszytkowska-Stawińska, M., De Clercq, E. & Balzarini, J.
     Synthesis and antiviral activity evaluation of acyclic 2’-azanucleosides bearing a phosphonomethoxy function in the side chain.
     Bioorg. Med. Chem., 17: 3756-3762 (2009).
     


277. Robins, M.J., Yang, H., Miranda, K., Peterson, M.A., De Clercq, E. & Balzarini, J.
     Synthesis and biological evaluation of 3,3-difluoropyridine-2,4(1H,3H)-dione and 3-deaza-3-fluorouracil base and nucleoside derivatives.
     J. Med. Chem., 52: 3018-3027 (2009).
     


278. Neyts, J., De Clercq, E., Singha, R., Chang, Y.H., Das, A.R., Chakraborty, S.K., Hong, S.C., Tsay, S.-C., Hsu, M.-H. & Hwu, J.R.
     Structure-activity relationship of new anti-hepatitis C virus agents: heterobicycle-coumarin conjugates.
     J. Med. Chem., 52: 1486-1490 (2009).
     


279. Xiong, Y.-z., Hu, H.-r., Chen, F.-e., Balzarini, J., Pannecouque, C. & De Clercq, E.
     Non-nucleoside reverse transcriptase inhibitors (part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
     Acta Pharm. Sinica, 44: 145-149 (2009).
     


280. De Palma, A.M., Thibaut, H.J., van der Linden, L., Lanke, K., Heggermont, W., Ireland, S., Andrews, R., Arimilli, M., Al-Tel, T.H., De Clercq, E., van Kuppeveld, F. & Neyts, J.
     Mutations in the nonstructural protein 3A confer resistance to the novel enterovirus replication inhibitor TTP-8307.
     Antimicrob. Agents Chemother., 53: 1850-1857 (2009).
     


281. De Clercq, E.
     Another ten stories in antiviral drug discovery (part C): “old” and “new” antivirals, strategies and perspectives.
     Med. Res. Rev., 29: 611-645 (2009).
     


282. De Clercq, E.
     Antiviral drug discovery: ten more compounds, and ten more stories (part B).
     Med. Res. Rev., 29: 571-610 (2009).
     


283. Paeshuyse, J., Letellier, C., Froeyen, M., Dutartre, H., Vrancken, R., Canard, B., De Clercq, E., Gueiffier, A., Teulade, J.-C., Herdewijn, P., Puerstinger, G., Koenen, F., Kerkhofs, P., Baraldi, P.G. & Neyts, J.
     A pyrazolotriazolopyrimidinamine inhibitor of bovine viral diarrhea virus replication that targets the viral RNA-dependent RNA polymerase.
     Antiviral Res., 82: 141-147 (2009).
     


284. Vliegen, I., Paeshuyse, J., De Burghgraeve, T., Lehman, L.S., Paulson, M., Shih, I.-H., Mabery, E., Boddeker, N., De Clercq, E., Reiser, H., Oare, D., Lee, W.A., Zhong, W., Bondy, S., Pürstinger, G. & Neyts, J.
     Substituted imidazopyridines as potent inhibitors of HCV replication.
     J. Hepatol., 50: 999-1009 (2009).
     


285. Sharma, D., Narasimhan, B., Kumar, P., Judge, V., Narang, R., De Clercq, E. & Balzarini, J.
     Synthesis, antimicrobial and antiviral evaluation of substituted imidazole derivatives.
     Eur. J. Med. Chem., 44: 2347-2353 (2009).
     


286. Santos, C.R., Capela, R., Pereira, C.S.G.P., Valente, E., Gouveia, L., Pannecouque, C., De Clercq, E., Moreira, R. & Gomes, P.
     Structure-activity relationships for dipeptide prodrugs of acyclovir : implications for prodrug design.
     Eur. J. Med. Chem., 44: 2339-2346 (2009).
     


287. Zhang, J., Liu, X. & De Clercq, E.
     Capsid (CA) protein as a novel drug target: recent progress in the research of HIV-1 CA inhibitors.
     Mini-Rev. Med. Chem., 9: 510-518 (2009).
     


288. Zoidis, G., Benaki, D., Myrianthopoulos, V., Naesens, L., De Clercq, E., Mikros, E. & Kolocouris, N.
     Synthesis of 1,2-annulated adamantane heterocycles: structural determination studies of a bioactive cyclic sulfite.
     Tetrahedron Lett., 50: 2671-2675 (2009).
     


289. De Clercq, E.
     The AMD3100 story: the path to the discovery of a stem cell mobilizer (Mozobil).
     Biochem. Pharmacol., 77: 1655-1664 (2009).
     


290. Duque, M.D., Camps, P., Profire, L., Montaner, S., Vázquez, S., Sureda, F.X., Mallol, J., López-Querol, M., Naesens, L., De Clercq, E., Prathalingam, S.R. & Kelly, J.M.
     Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines.
     Bioorg. Med. Chem., 17: 3198-3206 (2009).
     


291. Xiong, Y.Z., Chen, F.E., Balzarini, J., De Clercq, E. & Pannecouque, C.
     Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 13 : synthesis of fluorine-containing diaryltriazine derivatives for in vitro anti-HIV evaluation against wild-type strain.
     Chem. Biodivers., 6: 561-568 (2009).
     


292. Karki, S.S., Bahaduria, V.S., Rana, V., Kumar, S., Subbaro, P.G., Das, U., Balzarini, J., De Clercq, E. & Dimmock, J.R.
     1-Arylmethyl-2,3-dioxo-2,3-dihydroindole thiosemicarbazones as leads for developing cytotoxins and anticonvulsants.
     J. Enzyme Inhibition Med. Chem., 24: 537-544 (2009).
     


293. Khan, A., Nicholson, G., Greenman, J., Madden, L., McRobbie, G., Pannecouque, C., De Clercq, E., Ullom, R., Maples, D.L., Maples, R.L., Silversides, J.D., Hubin, T.J. & Archibald, S.J.
     Binding optimization through coordination chemistry: CXCR4 chemokine receptor antagonists from ultrarigid metal complexes.
     J. Am. Chem. Soc., 131: 3416-3417 (2009).
     


294. Andrei, G., De Clercq, E. & Snoeck, R.
     Drug targets in cytomegalovirus infection.
     Infect. Disord. Drug Targets, 9: 201-222 (2009)
     


295. Wang, Y., Liu, X.-y. & De Clercq, E.
     Role of the HIV-1 positive elongation factor P-TEFb and related inhibitors thereof.
     Mini Rev. Med. Chem., 9: 379-385 (2009).
     


296. De Clercq, E.
     Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.
     Int. J. Antimicrob. Agents, 33: 307-320 (2009).
     


297. Deng, B.-L., Zhao, Y., Hartman, T.L., Watson, K., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E. & Cushman, M.
     Synthesis of alkenyldiarylmethanes (ADAMS) containing the benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 44: 1210-1214 (2009).
     


298. Wang, Y.-P., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethyl-substituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 44: 1016-1023 (2009).
     


299. Zoidis, G., Kolocouris, N., Naesens, L. & De Clercq, E.
     Design and synthesis of 1,2-annulated adamantane piperidines with anti-influenza virus activity.
     Bioorg. Med. Chem., 17: 1534-1541 (2009).
     


300. Rajic, Z., Butula, I., Zorc, B., Kraljevic Pavelic, S., Hock, K., Pavelic, K., Naesens, L., De Clercq, E., Balzarini, J., Przyborowska, M., Ossowski, T. & Mintas, M.
     Cytostatic and antiviral activity evaluations of hydroxamic derivatives of some non-steroidal anti-inflammatory drugs.
     Chem. Biol. Drug Des., 73: 328-338 (2009).
     


301. Bannwarth, L., Rose, T., Dufau, L., Vanderesse, R., Dumont, J., Jamart-Grégoire, B., Pannecouque, C., De Clercq, E. & Reboud-Ravaux, M.
     Dimer disruption and monomer sequestration by alkyl tripeptides are successful strategies for inhibiting wild-type and multidrug-resistant mutated HIV-1 proteases.
     Biochemistry, 48: 379-387 (2009).
     


302. Yu, M., Liu, X. & De Clercq, E.
     NF-B: the inducible factors of HIV-1 transcription and inhibitors.
     Mini Rev. Med. Chem., 9: 60-69 (2009).
     


303. Cao, Y., Liu, X. & De Clercq, E.
     Cessation of HIV-1 transcription by inhibiting regulatory protein Rev-mediated RNA transport.
     Current HIV Res., 7: 101-108 (2009).
     


304. Wittine, K., Benci, K., Rajić, Z., Zorc, B., Kralj, M., Marjanović, M., Pavelić, K., De Clercq, E., Andrei, G., Snoeck, R., Balzarini, J. & Mintas, M.
     The novel phosphoramidate derivatives of NSAID 3-hydroxypropylamides: synthesis, cytostatic and antiviral activity evaluations.
     Eur. J. Med. Chem., 44: 143-151 (2009).
     


305. Pati, H.N., Das, U., Das, S., Bandy, B., De Clercq, E., Balzarini, J., Kawase, M., Sakagami, H., Quail, J.W., Stables, J.P. & Dimmock, J.R.
     The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1]octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones.
     Eur. J. Med. Chem., 44: 54-62 (2009).
     


306. De Clercq, E. & Neyts, J.
     Antiviral agents acting as DNA or RNA chain terminators.
     In: “Antiviral Strategies. Handbook of Experimental Pharmacology 189”, H.-G. Kräusslich & R. Bartenschlager (eds.). Springer-Verlag Berlin Heidelberg, pp. 53-84 (2009).
     



62 publications in the year 2008



307. Reddy, Y.T., Reddy, P.N., Crooks, P.A., De Clercq, E., Rao, G.V.P. & Rajitha, B.
     Synthesis and biological evaluation of novel substituted N1-[1-benzyl-3-(3-tert-butylcarbamoyl-octahydroisoquinolin-2yl)-2-hydroxy-propyl]-2-[(2-oxo-2H-chromene-3-carbonyl)amino] succinamide analogs as anti-viral and anti-HIV agents.
     Heterocyclic Communications, 14 : 419-426 (2008).
     


308. Selvam, P., Murugesh, N., Chandramohan, M., Pannecouque, C. & De Clercq, E.
     Synthesis, antiviral, and cytotoxic activities of 6-bromo/6,8-dibromo-4-(4-oxo-2-phenyl-4H-quinazolin-3-yl)-benzenesulphonamide.
     J. Appl. Chem. Res., 7: 18-23 (2008).
     


309. Rawal, R.K., Tripathi, R., Katti, S.B., Pannecouque, C. & De Clercq, E.
     Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
     Eur. J. Med. Chem., 43: 2800-2806 (2008).
     


310. Gammon, D.B., Snoeck, R., Fiten, P., Krečmerová, M., Holý, A., De Clercq, E., Opdenakker, G., Evans, D.H. & Andrei, G.
     Mechanism of antiviral drug resistance of vaccinia virus: Identification of residues in the viral DNA polymerase conferring differential resistance to antipoxvirus drugs.
     J. Virol., 82: 12520-12534 (2008).
     


311. Tatar, E., Küçükgüzel, I., De Clercq, E., Şahin, F. & Güllüce, M.
     Synthesis, characterization and screening of antimicrobial, antituberculosis, antiviral and anticancer activity of novel 1,3-thiazolidine-4-ones derived from 1-[2-(benzoylamino)-4-(methylthio)butyryl]-4-alkyl/arylakyl thiosemicarbazides.
     ARKIVOC, 191-210 (2008).
     


312. Camps, P., Duque, M.D., Vázquez, S., Naesens, L., De Clercq, E., Sureda, F.X., López-Querol, M., Camins, A., Pallàs, M., Prathalingam, S.R., Kelly, J.M., Romero, V., Ivorra, D. & Cortés, D.M.
     Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs.
     Bioorg. Med. Chem., 16: 9925-9936 (2008).
     


313. Yu, F., Liu, X., Zhan, P. & De Clercq, E.
     Recent advances in the research of HIV-1 RNase H inhibitors.
     Mini-Rev. Med. Chem., 8: 1243-1251 (2008).
     


314. Kolocouris, A., Spearpoint, P., Martin, S.R., Hay, A.J., López-Querol, M., Sureda, F.X., Padalko, E., Neyts, J. & De Clercq, E.
     Comparisons of the influenza A virus M2 channel binding affinities, anti-influenza virus potencies and NMDA antagonistic activities of 2-alkyl-2-aminoadamantanes and analogues.
     Bioorg. Med. Chem. Lett., 18: 6156-6160 (2008).
     


315. Lenaerts, L., De Clercq, E. & Naesens, L.
     Clinical features and treatment of adenovirus infections
     Rev. Med. Virol., 18: 357-374 (2008).
     


316. Véron, J.-B., Allouchi, H., Enguehard-Gueiffier, C., Snoeck, R., Andrei, G., De Clercq, E. & Gueiffier, A.
     Influence of 6- or 8-substitution on the antiviral activity of 3-arylalkylthiomethyl-imidazo[1,2-α]pyridine against human cytomegalovirus (CMV) and varicella-zoster virus (VZV): part II.
     Bioorg. Med. Chem., 16: 9536-9545 (2008).
     


317. Zhan, P., Liu, X., Cao, Y., Wang, Y., Pannecouque, C. & De Clercq, E.
     1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
     Bioorg. Med. Chem. Lett., 18: 5368-5371 (2008).
     


318. De Clercq, E.
     The discovery of antiviral agents: ten different compounds, ten different stories.
     Med. Res. Rev., 28: 929-953 (2008).
     


319. De Palma, A.M., Vliegen, I., De Clercq, E. & Neyts, J.
     Selective inhibitors of picornavirus replication
     Med. Res. Rev., 28: 823-884 (2008).
     


320. De Clercq, E.
     Antivirals: current state of the art.
     Future Virology, 3: 393-405 (2008).
     


321. Naesens, L., Andrei, G., Votruba, I., Krečmerová, M., Holý, A., Neyts, J., De Clercq, E. & Snoeck, R.
     Intracellular metabolism of the new antiviral compound 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine.
     Biochem. Pharmacol., 76: 997-1005 (2008).
     


322. De Clercq, E.
     Stand van zaken in verband met de therapie van AIDS.
     Tijdschr. Geneesk., 64: 807-813 (2008).
     


323. Gawin, R., De Clercq, E., Naesens, L. & Koszytkowska-Stawińska, M.
     Synthesis and antiviral evaluation of acyclic azanucleosides developed from sulphanilamide as a lead structure.
     Bioorg. Med. Chem., 16: 8379-8389 (2008).
     


324. Fogt, J., Januszczyk, P., Framski, G., Onishi, T., Izawa, K., De Clercq, E., Neyts, J. & Boryski, J.
     Synthesis and antiviral activity of novel derivatives of 2’-β-C-methylcytidine.
     Joint Symposium of the 18th International Round Table on Nucleosides, Nucleotides and Nucleic Acids and the 35th International Symposum on Nucleic Acids Chemistry, Kyoto, Japan, 8-12 September 2008.
     Nucleic Acids Symp. Series no. 52, 599-600 (2008).
     


325. Rai, D., Yadav, D., Balzarini, J., De Clercq, E. & Singh, R.K.
     Design and development of curcumin bioconjugates as antiviral agents.
     Joint Symposium of the 18th International Round Table on Nucleosides, Nucleotides and Nucleic Acids and the 35th International Symposum on Nucleic Acids Chemistry, Kyoto, Japan, 8-12 September 2008.
     Nucleic Acids Symp. Series no. 52, 599-600 (2008).
     


326. Yadav, D., Rai, D., Balzarini, J., De Clercq, E. & Singh, R.K.
     Thymidine analogs as potential antiviral agents.
     Joint Symposium of the 18th International Round Table on Nucleosides, Nucleotides and Nucleic Acids and the 35th International Symposum on Nucleic Acids Chemistry, Kyoto, Japan, 8-12 September 2008.
     Nucleic Acids Symp. Series no. 52, 263-264 (2008).
     


327. Selvam, P., Babu, K., Padamraj, R., Persoons, L. & De Clercq, E.
     Synthesis, antiviral and cytotoxic activities of some novel 2-phenyl-3-disubstituted quinazolin-4(3H)-ones.
     African J. Pharm. Pharmacol., 2: 110-115 (2008).
     


328. De Clercq, E.
     Emerging antiviral drugs.
     Expert Opin. Emerging Drugs, 13: 393-416 (2008).
     


329. Camps, P., Gómez, T., Munoz-Torrero, D., Rull, J., Sánchez, L., Boschi, F., Comes-Franchini, M., Ricci, A., Calvet, T., Font-Bardia, M., De Clercq, E. & Naesens, L.
     Synthesis and absolute configuration of novel N,O-psiconucleosides using (R)-N-phenylpantolactam as a resolution agent.
     J. Org. Chem., 73: 6657-6665 (2008).
     


330. De Clercq, E. & Field, H.J.
     Antiviral Chemistry & Chemotherapy’s current antiviral agents FactFile (2nd edition): Retroviruses.
     Antiviral Chem. Chemother., 19: 75-105 (2008).
     


331. De Clercq, E. & Field, H.J.
     Antiviral Chemistry & Chemotherapy’s current antiviral agents FactFile (2nd edition): RNA viruses.
     Antiviral Chem. Chemother., 19: 63-74 (2008).
     


332. Field, H.J. & De Clercq, E.
     Antiviral Chemistry & Chemotherapy’s current antiviral agents FactFile (2nd edition): DNA viruses.
     Antiviral Chem. Chemother., 19: 51-62 (2008).
     


333. Rawal, R.K., Tripathi, R., Kulkarni, S., Paranjape, R., Katti, S.B., Pannecouque, C. & De Clercq, E.
     2-(2,6-Dihalo-phenyl)-3-heteroaryl-2-ylmethyl-1,3-thiazolidin-4-ones: anti-HIV agents.
     Chem. Biol. Drug Des., 72: 147-154 (2008).
     


334. Zoidis, G., Tsotinis, A., Kolocouris, N., Kelly, J.M., Prathalingam, S.R., Naesens, L. & De Clercq, E.
     Design and synthesis of bioactive 1,2-annulated adamantane derivatives.
     Org. Biomol. Chem., 6: 3177-3185 (2008).
     


335. Monforte, A.-M., Rao, A., Logoteta, P., Ferro, S., De Luca, L., Barreca, M.L., Iraci, N., Maga, G., De Clercq, E., Pannecouque, C. & Chimirri, A.
     Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
     Bioorg. Med. Chem., 16: 7429-7435 (2008).
     


336. Alonso, N., Caamano, O., Fernández, F., Garcia-Mera, X., Morales, M., Rodriguez-Borges, J.E. & De Clercq, E.
     Synthesis and antiviral activities of novel purinyl- and pyrimidinyl-carbanucleosides derived from indan.
     Synthesis, 2008: 1845-1852 (2008).
     


337. Al-Soud, Y.A., Al-Masoudi, N.A., Schuppler, T., De Clercq, E. & Pannecouque, C.
     Microwave-assisted synthesis and anti-HIV activity of new acyclic C-nucleosides of 3-(D-ribo-tetritol-1-yl)-5-mercapto-1,2,4-triazoles. Part 1.
     Nucleosides Nucleotides Nucleic Acids, 27: 469-483 (2008).
     


338. Santos, C., Morais, J., Gouveia, L., De Clercq, E., Pannecouque, C., Nielsen, C.U., Steffansen, B., Moreira, R. & Gomes, P.
     Dipeptide derivatives of AZT: synthesis, chemical stability, activation in human plasma, hPEPT1 affinity, and antiviral activity.
     Chem. Med. Chem., 3: 970-978 (2008).
     


339. Zhan, P., Liu, X. & De Clercq, E.
     Recent advances in antiviral activity of benzo/heterothiadiazine dioxide derivatives.
     Curr. Med. Chem., 15: 1529-1540 (2008).
     


340. Dal Pozzo, F., Andrei, G., Daelemans, D., Winkler, M., Piette J., De Clercq, E. & Snoeck, R.
     Fluorescence-based antiviral assay for the evaluation of compounds against vaccinia virus, varicella zoster virus and human cytomegalovirus
     J. Virol. Methods, 151: 66-73 (2008).
     


341. Das, U., Doroudi, A., Das, S., Bandy, B., Balzarini, J., De Clercq, E. & Dimmock, J.R.
     E,E-2-Benzylidene-6-(nitrobenzylidene)cyclohexanones: syntheses, cytotoxicity and an examination of some of their electronic, steric and hydrophobic properties.
     Bioorg. Med. Chem., 16: 6261-6268 (2008).
     


342. Xiong, Y.-Z., Chen, F.-E., Balzarini, J., De Clercq, E. & Pannecouque, C.
     Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: Structural modulations of diaryltriazines with potent anti-HIV activity.
     Eur. J. Med. Chem., 43: 1230-1236 (2008).
     


343. Dzimbeg, G., Zorc, B., Kralj, M., Ester, K., Pavelić, K., Andrei, G., Snoeck, R., Balzarini, J., De Clercq, E. & Mintas, M.
     The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations.
     Eur. J. Med. Chem., 43: 1180-1187 (2008).
     


344. Pati, H.N., Das, U., Kawase, M., Sakagami, H., Balzarini, J., De Clercq, E. & Dimmock, J.R.
     1-Aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides and related adducts: a quest for selective cytotoxicity for malignant cells.
     Bioorg. Med. Chem., 16: 5747-5753 (2008).
     


345. Perković, I., Butula, I., Zorc, B., Hock, K., Kraljević Pavelić, S., Pavelić, K, De Clercq, E., Balzarini, J. & Mintas, M.
     Novel lipophilic hydroxyurea derivatives: synthesis, cytostatic and antiviral activity evaluations.
     Chem. Biol. Drug Des., 71: 546-553 (2008).
     


346. De Palma, A.M., Heggermont, W., Lanke, K., Coutard, B., Bergmann, M., Monforte, A.-M., Canard, B., De Clercq, E., Chimirri, A., Pürstinger, G., Rohayem, J., van Kuppeveld, F. & Neyts, J.
     The thiazolobenzimidazole TBZE-029 inhibits enterovirus replication by targeting a short region immediately downstream from motif C in the non-structural protein 2C.
     J. Virol., 82: 4720-4730 (2008).
     


347. Tomassi, C., Nguyen Van Nhien, A., Marco-Contelles, J., Balzarini, J., Pannecouque, C., De Clercq, E. & Postel, D.
     Synthesis and anti-HIV1 biological activity of novel 5”-ATSAO compounds.
     Bioorg. Med. Chem., 16: 4733-4741 (2008).
     


348. Perjési, P., Das, U., De Clercq, E., Balzarini, J., Kawase, M., Sakagami, H., Stables, J.P., Lorand, T., Rozmer, Z. & Dimmock, J.R.
     Design, synthesis and antiproliferative activity of some 3-benzylidene-2,3-dihydro-1-benzopyran-4-ones which display selective toxicity for malignant cells.
     Eur. J. Med. Chem, 43: 839-845 (2008).
     


349. Wang, Y.-P., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonyl-methylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Bioorg. Med. Chem., 16: 3887-3894 (2008).
     


350. Liu, X.-y., Yan, R.-z., Wang, Y., Zhan, P., De Clercq, E., Pannecouque, C., Witvrouw, M., Molina, M.T. & Vega, S.
     Synthesis and anti-HIV activity evaluation of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo[4,5-e][1,2,4]thiadiazines.
     Arch. Pharm. Chem. Life Sci., 341: 216-222 (2008).
     


351. De Palma, A.M., Pürstinger, G., Wimmer, E., Patick, A.K., Andries, K., Rombaut, B., De Clercq, E. & Neyts, J.
     Potential use of antiviral agents in polio eradication.
     Emerging Infect. Dis., 14: 545-551 (2008).
     


352. Lagoja, I.M. & De Clercq, E.
     Anti-influenza virus agents: synthesis and mode of action.
     Med. Res. Rev., 28: 1-38 (2008).
     


353. Tomassi, C., Nguyen Van Nhien, A., Marco-Contelles, J., Balzarini, J., Pannecouque, C., De Clercq, E., Soriano, E. & Postel, D.
     Synthesis, anti-HIV-1 activity, and modeling studies of N-3 Boc TSAO compound.
     Bioorg. Med. Chem. Lett., 18: 2277-2281 (2008).
     


354. Lenaerts, L., Kelchtermans, H, Geboes, L., Matthys, P., Verbeken, E., De Clercq, E. & Naesens, L.
     Recovery of humoral immunity is critical for successful antiviral therapy in disseminated mouse adenovirus type 1 infection.
     Antimicrob. Agents Chemother., 52: 1462-1471 (2008).
     


355. Ptak, R.G., Gallay, P.A., Jochmans, D., Halestrap, A.P., Ruegg, U.T., Pallansch, L.A., Bobardt, M.D., de Béthune, M.-P., Neyts, J., De Clercq, E., Dumont, J.-M., Scalfaro, P., Besseghir, K., Wenger, R.M. & Rosenwirth, B.
     Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent.
     Antimicrob. Agents Chemother., 52: 1302-1317 (2008).
     


356. Leyssen, P., De Clercq, E. & Neyts, J.
     Molecular strategies to inhibit the replication of RNA viruses.
     In: Special Issue on “Treatment of Highly Pathogenic RNA Viral Infections”, Bray, M. & Neyts, J., eds.
     Antiviral Res., 78: 9-25 (2008).
     


357. Pannecouque, C., Daelemans, D. & De Clercq, E.
     Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later.
     Nature Protocols, 3: 427-434 (2008).
     


358. Cullen, M.D., Cheung, Y.-F., Houslay, M.D., Hartman, T.L., Watson, K.M., Buckheit Jr., R.W., Pannecouque, C., De Clercq, E. & Cushman, M.
     Investigatino of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
     Bioorg. Med. Chem. Lett., 18: 1530-1533 (2008).
     


359. Küçükgüzel, I., Tatar, E., Küçükgüzel, S.G., Rollas, S. & De Clercq, E.
     Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents.
     Eur. J. Med. Chem., 43: 381-392 (2008).
     


360. Andrei, G., De Clercq, E., & Snoeck, R.
     Novel inhibitors of human CMV.
     Curr. Opin. Invest. Drugs, 9: 132-145 (2008).
     


361. Wang, Y., Chen, F.-E., Balzarini, J., De Clercq, E. & Pannecouque, C.
     Non-nucleoside HIV-1 reverse-transcriptase inhibitors. Part 10 : Synthesis and anti-HIV activity of 5-alkyl-6-(1-naphthylmethyl)pyrimidin-4(3H)-ones with a mono- or disubstituted 2-amino function as novel 'dihydro-alkoxy-benzyl-oxopyrimidine' (DABO) analogues.
     Chemistry & Biodiversity, 5: 168-176 (2008).
     


362. Ferir, G., Kaptein, S., Neyts, J. & De Clercq, E.
     Antiviral treatment of chronic hepatitis B virus infections: the past, the present and the future.
     Rev. Med. Virol., 18: 19-34 (2008).
     


363. Hwu, J.R., Singha, R., Hong, S.C., Chang, Y.H., Das, A.R., Vliegen, I., De Clercq, E. & Neyts, J.
     Synthesis of new benzimidazole-coumarin conjugates as anti-hepatitis C virus agents.
     Antiviral Res., 77: 157-162 (2008).
     


364. Cullen, M.D., Sarkar, T., Hamel, E., Hartman, T.L., Watson, K.M., Buckheit Jr., R.W., Pannecouque, C., De Clercq, E. & Cushman, M.
     Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
     Bioorg. Med. Chem. Lett., 18: 469-473 (2008).
     


365. Aubin, Y., Audran, G., Monti, H. & De Clercq, E.
     Chemoenzymatic synthesis and antiviral evaluation of conformationally constrained and 3'-methyl-branched carbanucleosides using both enantiomers of the same building block.
     Bioorg. Med. Chem., 16: 374-381 (2008).
     


366. Lin, Y., Liu, X., Yan, R., Li, J., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][2,1,2,6]thiadiazin-4-(3H)-one 2,2-dioxides (TTDDs).
     Bioorg. Med. Chem., 16: 157-163 (2008).
     


367. De Clercq, E.
     The design of drugs for HIV and HCV.
     Nature Rev. Drug Discovery, 6: 1001-1018 (2007).
     Supplement to Nature Publishing Group, Nature Biotechnology and Nature Reviews Drug Discovery, S91-S108 (2008).
     


368. De Clercq, E.
     Three decades of antiviral drugs (Editorial).
     Nature Rev. Drug Discovery, 6: 941 (2007).
     Supplement to Nature Publishing Group, Nature Biotechnology and Nature Reviews Drug Discovery, S3 (2008).
     



85 publications in the year 2007



369. Ali, M.A., Yar, M.S., Siddiqui, A.A., Sriram, D., Yogeeswari, P. & De Clercq, E.
     Synthesis and anti-HIV activity of N'-nicotinoyl--3-(4'-hydroxy-3'-methylphenyl)-5-[substituted phenyl]-2-pyrazolines.
     Acta Pol. Pharm., 64: 423-428 (2007).
     


370. Mehellou, Y. & De Clercq, E.
     The current status of HIV chemotherapy.
     IBScientific Journal of Science, 2: 44-56 (2007).
     


371. Snoeck, R., Andrei, G. & De Clercq, E.
     Therapy of poxvirus infections.
     In: Poxviruses. Mercer, A., Schmidt, A. & Weber, O., eds. Birkhäuser Verlag, Basel, Switzerland, pp. 375-395 (2007).
     


372. Al-Soud, Y.A., Al-Masoudi, N.A., De Clercq, E. & Pannecouque, C.
     Nitroimidazoles, part 4: synthesis and anti-HIV activity of new 5-alkylsulfanyl and 5-(4’-arylsulfonyl)piperazinyl-4-nitroimidazole derivatives.
     Heteroatom Chem., 18: 333-340 (2007).
     


373. Ali, M.A., Shaharyar, M. & De Clercq, E.
     Synthesis of 5-(4-hydroxy-3-methylphenyl) -5- (substituted phenyl)-4, 5-dihydro-1H-1-pyrazolyl-4-pyridylmethanone derivatives with anti-viral activity.
     J. Enzyme Inhib. Med. Chem., 22: 702-708 (2007).
     


374. Patel, R.B., Chikhalia, K.H., Pannecouque, C. & De Clercq, E.
     Synthesis of novel PETT analogues: 3,4-dimethoxy phenyl ethyl 1,3,5-triazinyl thiourea derivatives and their antibacterial and anti-HIV studies
     J. Braz. Chem. Soc., 18: 312-321 (2007).
     


375. Duraffour, S., Snoeck, R., de Vos, R., van Den Oord, J.J., Crance, J.-M., Garin, D., Hruby, D.E., Jordan, R., De Clercq, E. & Andrei, G.
     Activity of the anti-orthopoxvirus compound ST-246 against vaccinia, cowpox and camelpox viruses in cell monolayers and organotypic raft cultures.
     Antiviral Ther., 12: 1205-1216 (2007).
     


376. Al-Soud, Y.A., Al-Masoudi, N.A., Hassan, H.G., De Clercq, E. & Pannecouque, C.
     Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives.
     Acta Pharm., 57: 379-393 (2007).
     


377. Etheve-Quelquejeu, M., Tranchier, J.-P., Rose-Munch, F., Rose, E., Naesens, L. & De Clercq, E.
     6-(Arene)tricarbonylchromium and manganese complexes linked to 2’-deoxyuridine.
     Organometallics, 26: 5727-5730 (2007).
     


378. Maruyama, T., Demizu, Y., Kozai, S., Witvrouw, M., Pannecouque, C., Balzarini, J., Snoeck, R., Andrei, G. & De Clercq, E.
     Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.
     Proceedings of the XVII International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Bern, Switzerland, 3-7 September 2006.
     Nucleosides, Nucleotides & Nucleic Acids, 26: 1553-1558 (2007).
     


379. Jahnz-Wechmann, Z., Boryski, J., Izawa, K., Onishi, T., Neyts, J. & De Clercq, E.
     New analogs of acyclovir substituted at the side chain.
     Proceedings of the XVII International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Bern, Switzerland, 3-7 September 2006.
     Nucleosides, Nucleotides & Nucleic Acids, 26: 917-920 (2007).
     


380. Garozzo, A., Cutrì, C.C., Pannecouque, C., Castro, A., Guerrera, F. & De Clercq, E.
     Isothiazole derivatives as antiviral agents.
     Antiviral Chem. Chemother., 18: 277-283 (2007).
     


381. Pérez-Castro, I., Caamaňo, O., Fernández, F., Garcia, M.D., López, C. & De Clercq, E.
     Synthesis of 4-substituted-1,2,3-triazole carbanucleoside analogues of ribavirin via click chemistry.
     Org. Biomol. Chem., 5: 3805-3813 (2007).
     


382. Duraffour, S., Snoeck, R., Krečmerová, M., van Den Oord, J., De Vos, R., Holý, A., Crance, J.M., Garin, D., De Clercq, E. & Andrei, G.
     Activities of several classes of acyclic nucleoside phosphonates against camelpox virus replication in different cell culture models.
     Antimicrob. Agents Chemother., 51: 4410-4419 (2007).
     


383. McRobbie, G., Valks, G.C., Empson, C.J., Khan, A., Silversides, J.D., Pannecouque, C., De Clercq, E., Fiddy, S.G., Bridgeman, A.J., Young, N.A. & Archibald, S.J.
     Probing key coordination interactions: configurationally restricted metal activated CXCR4 antagonists.
     Dalton Transactions, 5008-5018 (2007).
     


384. Krečmerová, M., Holý, A., Pohl, R., Masojíkková, M., Andrei, G., Naesens, L., Neyts, J., Balzarini, J., De Clercq, E. & Snoeck, R.
     Ester prodrugs of cyclic 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine: synthesis and antiviral activity.
     J. Med. Chem., 50: 5765-5772 (2007).
     


385. Trivedi, J.C., Bariwal, J.B., Upadhyay, K.D., Naliapara, Y.T., Joshi, S.K., Pannecouque, C., De Clercq, E. & Shay, A.K.
     Improved and rapid synthesis of new coumarinyl chalcone derivatives and their antiviral activity.
     Tetrahedron Lett., 48: 8472-8474 (2007).
     


386. Wu, J., Liu, X., Cheng, X., Cao, Y., Wang, D., Li, Z., Xu, W., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs.
     Molecules, 12: 2003-2016 (2007).
     


387. Tušek-Božić, L., Juribašić, M., Komac, M., Cmrečki, V., Zrinski, I., Balzarini, J. & De Clercq, E.
     Eco-friendly synthesis and biological evaluation of new quinoline-based dialkyl α-aminophosphonates.
     Lett Org. Chem., 4: 332-338 (2007).
     


388. De Clercq, E.
     Existing influenza antivirals: their mechanisms of action and potential in the face of avian influenza.
     In: Combating the Threat of Pandemic Influenza: Drug Discovery Approaches. Torrence, P.F., ed. John Wiley & Sons, Inc., Hoboken, New York, USA,pp. 1-37 (2007).
     


389. Al-Masoudi, N.A., Al-Soud, Y.A., De Clercq, E. & Pannecouque, C.
     Nitroimidazoles. Part 6. Synthesis, structure and in vitro anti-HIV activity of new 5-substituted piperazinyl-4-nitroimidazole derivatives.
     Antiviral Chem. Chemother., 18: 191-200 (2007).
     


390. Véron, J.-B., Enguehard-Gueiffier, C., Snoeck, R., Andrei, G., De Clercq, E. & Gueiffier, A.
     Influence of 6 or 8-substitution on the antiviral activity of 3-phenethylthiomethylimidazo[1,2-a]pyridine against human cytomegalovirus (HCMV) and varicella-zoster virus (VZV).
     Bioorg. Med. Chem., 15: 7209-7219 (2007).
     


391. Cullen, M.D., Deng, B.-L., Hartman, T.L., Watson, K.M., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E. & Cushman, M.
     Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
     J. Med. Chem., 50: 4854-4867 (2007).
     


392. Paeshuyse, J., Chezal, J.-M., Froeyen, M., Leyssen, P., Dutartre, H., Vrancken, R., Canard, B., Letellier, C., Li, T., Mittendorfer, H., Koenen, F., Kerkhofs, P., De Clercq, E., Herdewijn, P., Puerstinger, G., Gueiffier, A., Chavignon, O., Teulade, J.-C. & Neyts, J.
     The imidazopyrrolopyridine analogue AG110 is a novel, highly selective inhibitor of pestiviruses that targets the viral RNA-dependent RNA polymerase at a hot spot for inhibition of viral replication?
     J. Virol., 91: 11046-11053 (2007).
     


393. Painter, G.R., Almond, M.R., Trost, L.C., Lampert, B.M., Neyts, J., De Clercq, E., Korba, B.E., Aldern, K.A., Beadle, J.R. & Hostetler, K.Y.
     Evaluation of hexadecyloxypropyl-9-R-[2-(phosphonomethoxy)propyl]adenine, CMX157, as a potential treatment for human immunodeficiency virus type 1 and hepatitis B virus infections.
     Antimicrob. Agents Chemother., 51: 3505-3509 (2007).
     


394. Karki, S.S., Thota, S., Darj, S.Y., Balzarini, J. & De Clercq, E.
     Synthesis, anticancer, and cytotoxic activities of some mononuclear Ru(II) compounds.
     Bioorg. Med. Chem., 15: 6632-6641 (2007).
     


395. Youssef, D., Nichols, C.E., Cameron, T.S., Balzarini, J., De Clercq, E. & Jha, A.
     Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues.
     Bioorg. Med. Chem. Lett., 17: 5624-5629 (2007).
     


396. Koszytkowska-Stawińska, M., Kolaczkowska, E., Adamkiewicz, E. & De Clercq, E.
     Synthesis and antiviral properties of aza-analogues of ganciclovir derived from 5,5-bis(hydroxymethyl)pyrrolidin-2-one.
     Tetrahedron, 63: 10587-10595 (2007).
     


397. Andrei, G., Fiten, P., Froeyen, M., De Clercq, E., Opdenakker, G. & Snoeck, R.
     DNA Polymerase mutations in drug-resistant herpes simplex mutants determine in vivo neurovirulence and drug-enzyme interactions.
     Antiviral Ther., 12: 719-732 (2007).
     


398. Puerstinger, G., Paeshuyse, J., Heinrich, S., Mohr, J., Schraffl, N., De Clercq, E. & Neyts, J.
     Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: further optimization of anti-hepatitis C virus activity.
     Bioorg. Med. Chem. Lett., 17: 5111-5114 (2007).
     


399. Gazivoda, T., Šokčević, M., Kralj, M., Šuman, L., Pavelić, K., De Clercq, E., Andrei, G., Snoeck, R., Balzarini, J., Mintas, M. & Raić-Malić, S.
     Synthesis and antiviral and cytostatic evaluations of the new C-5 substituted pyrimidine and furo[2,3-d]pyrimidine 4’,5’-didehydro-L-ascorbic acid derivatives.
     J. Med. Chem., 50, 4105-4112 (2007).
     


400. Jarrahpour, A., Khalili, D., De Clercq, E., Salmi, C. & Brunel, J.M.
     Synthesis, antibacterial, antifungal and antiviral activity evaluation of some new bis-Schiff bases of isatin and their derivatives.
     Molecules, 12: 1720-1730 (2007).
     


401. De Clercq, E.
     
     In: Advances in Antiviral Drug Design. Vol. 5. De Clercq, E., ed. Elsevier Science N.V., London, United Kingdom, pp. 59-112 (2007).
     


402. De Clercq, E.
     Status presens of antiviral drugs and strategies: Part I: DNA viruses and retroviruses.
     In: Advances in Antiviral Drug Design. Vol. 5. De Clercq, E., ed. Elsevier Science N.V., London, United Kingdom, pp. 1-58 (2007).
     


403. Robins, M.J., Nowak, I., Rajwanshi, V.K., Miranda, K., Cannon, J.F., Peterson, M.A., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis and antiviral evaluation of 6-(alkyl-heteroaryl)furo[2,3-d]pyrimidin-2(3H)-one nucleosides and analogues with ethynyl, ethenyl, and ethyl spacers at C6 of the furopyrimidine core.
     J. Med. Chem., 50: 3897-3905 (2007).
     


404. Bang Kang, S., De Clercq, E. & Lakshman, M.K.
     Pd-catalyzed C-C bond-forming reactions of thymidine mesitylene sulfonate.
     J. Org. Chem., 72: 5724-5730 (2007).
     


405. Jha, A., Mukherjee, C., Prasad, A.K., Parmar, V.S., De Clercq, E., Balzarini, J., Stables, J.P., Manavathu, E.K., Shrivastav, A., Sharma, R.K., Nienaber, K.H., Zello, G.A. & Dimmock, J.R.
     E,E,E-1-(4-Arylamino-4-oxo-2-butenoyl)-3,5-bis(arylidene)-4-piperidones: a topographi-cal study of some novel potent cytotoxins.
     Bioorg. Med. Chem., 15: 5854-5865 (2007)
     


406. Jha, A., Mukherjee, C., Rolle, A.J., De Clercq, E., Balzarini, J. & Stables, J.P.
     Cytostatic activity of novel 4’-aminochalcone-based imides.
     Bioorg. Med. Chem. Lett., 17: 4545-4550 (2007).
     


407. Rawal, R.K., Tripathi, R.K., Katti, S.B., Pannecouque, C. & De Clercq, E.
     Synthesis and biological evaluation of 2,3-diarylsubstituted-1,3-thiazolidin-4-ones as anti-HIV agents.
     Med. Chem., 3: 355-363 (2007).
     


408. Kolocouris, N., Zoidis, G., Foscolos, G.B., Fytas, G., Prathalingham, S.R., Kelly, J.M., Naesens, L. & De Clercq, E.
     Design and synthesis of bioactive adamantane spiro heterocycles.
     Bioorg. Med. Chem. Lett., 17: 4358-4362 (2007).
     


409. Sakamoto, T., Cullen, M.D., Hartman, T.L., Watson, K.M., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E. & Cushman, M.
     Synthesis and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems.
     J. Med. Chem., 50: 3314-3321 (2007).
     


410. Rajkapoor, B., Murugesh, N., Kavimani, S., Krishna, D.R., Ravichandran, V., Gobinath, M., Harikrishnan, N., Vidyasagar, J., De Clercq, E. & Franzblau, S.G.
     Antimycobacterial, antiviral and cytotoxic studies of Indigofera aspalathoides Vahl.
     Phcog. Mag., 3: 163-166 (2007).
     


411. Shi, M., Wang, X., De Clercq, E., Takao, S. & Baba, M.
     Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
     Antimicrob. Agents Chemother., 51: 2600-2604 (2007).
     


412. Bugatti, A., Urbinati, C., Ravelli, C., Arthos, J., De Clercq, E., Liekens, S. & Rusnati, M.
     Heparin-mimicking sulfonic acid polymers as multitarget inhibitors of human immunodeficiency virus type 1 Tat and gp120 proteins.
     Antimicrob. Agents Chemother., 51: 2337-2345 (2007).
     


413. Prekupec, S., Makuc, D., Plavec, J., Suman, L., Kralj, M., Pavelić, K., Balzarini, J., De Clercq, E., Mintas, M. & Raić-Malić, S.
     Novel C-6 fluorinated acyclic side chain pyrimidine derivatives: synthesis, 1H and 13C NMR conformational studies, and antiviral and cytostatic evaluations.
     J. Med. Chem., 50: 3037-3045 (2007).
     


414. Kücükgüzel, S.G., Kücükgüzel, I., Tatar, E., Rollas, S., Şahin, F., Güllüce, M., De Clercq, E. & Kabasaka, L.
     Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.
     Eur. J. Med. Chem., 42: 893-901 (2007).
     


415. Stevens, M., Balzarini, J., Lagoja, I., Noppen, B., François, K., Van Aerschot, A., Herdewijn, P., De Clercq, E. & Pannecouque, C.
     Inhibition of human immunodeficiency virus type 1 transcription by N-aminoimidazole derivatives.
     Virology, 365: 220-237 (2007).
     


416. Cristofoli, W.A., Wiebe, L.I., De Clercq, E., Andrei, G., Snoeck, R., Balzarini, J. & Knaus, E.E.
     5-Alkynyl analogs of arabinouridine and 2’-deoxyuridine: cytostatic activity against herpes simplex virus and varicella-zoster thymidine kinase gene-transfected cells.
     J. Med. Chem., 50: 2851-2857 (2007).
     


417. Moukha-Chafiq, O., Taha, M.L., Mouna, A., Lazrek, H.B., Vasseur, J.-J. & De Clercq, E.
     Synthesis and biological evaluation of some α-[6-(1’-carbamoylalkylthio)-1-H-pyrazolo[3,4-D]pyrimidin-4-yl]thioalkylcarboxamide acyclonucleosides.
     Nucleosides, Nucleotides & Nucleic Acids, 26: 335-345 (2007).
     


418. De Clercq, E. & Neyts, J.
     Avian influenza A (H5N1) infection: targets and strategies for chemotherapeutic intervention.
     Trends Pharmacol. Sci., 28: 280-285 (2007).
     


419. Lebeau, I., Andrei, G., Krečmerová, M., De Clercq, E., Holý, A. & Snoeck, R.
     Inhibitory activities of three classes of acyclic nucleoside phosphonates against murine polyomavirus and primate simian virus 40 strains.
     Antimicrob. Agents Chemother., 51: 2268-2273 (2007).
     


420. Al-Masoudi, N.A., Al-Soud, Y.A., Ali, I.A., Schuppler, T., Pannecouque, C. & De Clercq, E.
     New AZT analogues having 5’-alkylsulfonyl groups: synthesis and anti-HIV activity.
     Nucleosides, Nucleotides & Nucleic Acids, 26: 223-230 (2007).
     


421. González-Díaz, H., Bonet, I., Terán, C., De Clercq, E., Bello, R., García, M.M., Santana, L. & Uriarte, E.
     ANN-QSAR model for selection of anticancer leads from structurally heterogeneous series of compounds.
     Eur. J. Med. Chem., 42: 580-585 (2007).
     


422. Kumar, V.N., De Clercq, E. & Rajitha, B.
     One-pot synthesis of novel 3-(2-oxo-2H-chromen-3-yl)-[1,3,4]thiadiazino [2,3-b]quinazolin-6 (2H)-ones under microwave irradiation.
     Phosphorys, Sulfur, and Silicon, 182: 273-279 (2007).
     


423. Zhang, Z., Amer, A., Fan, X., Balzarini, J., Neyts, J., De Clercq, E., Prichard, M., Kern, E. & Torrence, P.F.
     Synthesis and antiviral activities of new acyclic and “double-headed” nucleoside analogues.
     Bioorg. Chem., 35: 221-232 (2007).
     


424. Andrei, G., Fiten, P., Goubau, P., van Landuyt, H., Gordts, B., Selleslag, D., De Clercq, E., Opdenakker, G. & Snoeck, R.
     Dual infection with polyomavirus BK and acyclovir-resistant herpes simplex virus successfully treated with cidofovir in a bone marrow transplant recipient.
     Transpl. Infect. Dis., 9: 126-131 (2007).
     


425. De Clercq, E.
     Anti-HIV drugs.
     Verh. K. Acad. Geneesk. Belg., 69: 81-104 (2007).
     


426. De Clercq, E.
     AIDS in the Third World: How to stop the HIV infection ?
     Verh. K. Acad. Geneesk. Belg., 69: 65-80 (2007).
     


427. Dal Pozzo, F., Andrei, G., Lebeau, I., Beadle, J.R., Hostetler, K.Y., De Clercq, E. & Snoeck, R.
     In vitro evaluation of the anti-orf virus activity of alkoxyalkyl esters of CDV, cCDV and (S)-HPMPA.
     Antiviral Res., 75: 52-57 (2007).
     


428. De Clercq, E.
     The acyclic nucleoside phosphonates from their inception to clinical use: historical perspective.
     Antiviral Res., 75: 1-13 (2007).
     


429. Ji, L., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or α-cyanoarylmethl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
     J. Med. Chem., 50: 1778-1786 (2007).
     


430. Huang, W., Miller, M.J., De Clercq, E. & Balzarini, J.
     Syntheses and anti-HIV activities of (±)-norcarbovir and (±)-norabacavir.
     Org. Biomol. Chem., 5: 1164-1166 (2007).
     


431. Rawal, R.K., Tripathi, R., Katti, S.B., Pannecouque, C. & De Clercq, E.
     Synthesis and evaluation of 2-(2,6-dihalophenyl)-3-pyrimidinyl-1,3-thiazolidin-4-one analogues as anti-HIV-1 agents.
     Bioorg; Med. Chem. Lett., 15: 3134-3142 (2007).
     


432. Daelemans, D., Lu, R., De Clercq, E. & Engelman, A.
     Characterization of a replication-competent, integrase-defective human immunodeficiency virus (HIV)/simian virus 40 chimera as a powerful tool for the discovery and validation of HIV integrase inhibitors.
     J. Virol., 81: 4381-4385 (2007).
     


433. Stevens, M., Pollicita, M., Pannecouque, C., Verbeken, E., Tabarrini, O., Cecchetti, V., Aquaro, S., Perno, C.F., Fravolini, A., De Clercq, E., Schols, D. & Balzarini, J.
     Novel in vivo model for the study of human immunodeficiency virus type 1 transcription inhibitors: evaluation of new 6-desfluoroquinolone derivatives.
     Antimicrob. Agents Chemother., 51: 1407-1413 (2007).
     


434. Hatse, S., Huskens, D., Princen, K., Vermeire, K., Bridger, G.J., De Clercq, E., Rosenkilde, M.M., Schwartz, T.W. & Schols, D.
     Modest human immunodeficiency virus coreceptor function of CXCR3 is strongly enhanced by mimicking the CXCR4 ligand binding pocket in the CXCR3 receptor.
     J. Virol., 81: 3632-3639 (2007).
     


435. Barreca, M.L., Rao, A., De Luca, L., Iraci, N., Monforte, A.-M., Maga, G., De Clercq, E., Pannecouque, C., Balzarini, J. & Chimirri, A.
     Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
     Bioorg. Med. Chem. Lett., 17: 1956-1960 (2007).
     


436. Krečmerová, M., Holý, A., Pískala, A., Masojídková, Andrei, G., Naesens, L., Neyts, J., Balzarini, J., De Clercq, E. & Snoeck, R.
     Antiviral activity of triazine analogues of 1-(S)-[3-hydroxy-2-(phosphonomethoxy)-propyl]cytosine (cidofovir) and related compounds.
     J. Med. Chem., 50: 1068-1077 (2007).
     


437. Harinantenaina, L., Asakawa, Y. & De Clercq, E.
     Cinnamacrins A-C, cinnafragin D, and cytostatic metabolites with α-glucoside inhibitory activity from Cinnamosma macrocarpa.
     J. Nat. Products, 70: 277-282 (2007).
     


438. De Clercq, E.
     Acyclic nucleoside phosphonates: past, present and future. Bridging chemistry to HIV, HBV, HCV, HPV, adeno-, herpes-, and poxvirus infections: the phosphonate bridge.
     Biochem. Pharmacol., 73: 911-922 (2007).
     


439. Ji, L., Chen, F.-E., Xie, B., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Synthesis and anti-HIV activity evaluation of 1-[(alkenyl or alkynyl or alkyloxy)methyl]-5-alkyl-6-(1-naphthoyl)-2,4-pyrimidinediones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Eur. J. Med. Chem., 42: 198-204 (2007).
     


440. Pati, H.N., Das, U., De Clercq, E., Balzarini, J. & Dimmock, J.R.
     Molecular modifications of 2-arylidene-1-indanones leading to increased cytotoxic potencies.
     J. Enzyme Inhibition Med. Chem., 22: 37-42 (2007).
     


441. Ying, C., Colonno, R.J., De Clercq, E. & Neyts, J.
     Ribavirin and mycophenolic acid markedly potentiate the anti-hepatitis B virus activity of entecavir.
     Antiviral Res., 73: 192-196 (2007).
     


442. Liekens, S., Gijsbers, S., Vanstreels, E., Daelemans, D., De Clercq, E. & Hatse, S.
     The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling, and induces apoptosis in FGF2-overexpressing endothelial cells.
     Mol. Pharmacol., 71: 695-703 (2007).
     


443. Siddiqui, A.A., Rajesh, R., Majahid-Ul I., Alagarsamy, V. & De Clercq, E.
     Synthesis, antiviral, antituberculostic, and antibacterial activities of some novel, 4-(4-substituted phenyl)-6-(4-nitrophenyl)-2-(substituted imino) pyrimidines.
     Arch. Pharm., 340: 95-102 (2007).
     


444. Bonatti, H., Aigner, F., De Clercq, E., Boesmüller, C., Widschwendner, A., Larcher, C., Margreiter, R. & Schneeberger, S.
     Local administration ofl cidofovir for human papilloma virus associated skin lesions in transplant recipients.
     Transpl. Int., 20: 238-246 (2007).
     


445. Das, U., Alcorn, J., Shrivastav, A., Sharma, R.K., De Clercq, E., Balzarini, J. & Dimmock, J.R.
     Design, synthesis and cytotoxic properties of novel 1-[4-(2-alkylaminoethoxy)-phenylcarbonyl]-3,5-bis(arylidene)-4-piperidones and related compounds.
     Eur. J. Med. Chem., 42: 71-80 (2007).
     


446. De Clercq, E.
     Viruses and viral diseases
     In: “Comprehensive Medicinal Chemistry II”, vol. 7. Taylor, J.B. & Triggle, D.J., eds. Elsevier Science Ltd, United Kingdom, pp. 253-293 (2007).
     


447. Koszytkowska-Stawinska, M., Kaleta, K., Sas, W. & De Clercq, E.
     Synthesis and antiviral properties of aza-analogues of acyclovir.
     Nucleosides, Nucleotides, Nucleic Acids, 26: 51-64 (2007).
     


448. Tataridis, D.; Fytas, G.; Kolocouris, A.; Fytas, C.; Kolocouris, N.; Foscolos, G.B.; Padalko, E.; Neyts, J., De Clercq, E.
     Influence of an additional 2-amino substituent of the 1-aminoethyl pharmacophore group on the potency of rimantadine against influenza virus A.
     Bioorg. Med. Chem. Lett., 17: 692-696 (2007).
     


449. Rawal, R.K., Tripathi, R.K., Katti, S.B., Pannecouque, C. & De Clercq, E.
     Design, synthesis, and evaluation of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
     Bioorg. Med. Chem., 15: 1725-1731 (2007).
     


450. Puerstinger, G., Paeshuyse, J., De Clercq, E. & Neyts, J.
     Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: from anti-pestivirus to anti-hepatitis C virus activity.
     Bioorg. Med. Chem. Lett., 17: 390-393 (2007).
     


451. De Palma, A.M., Heggermont, W., Leyssen, P., Pürstinger, G., Wimmer, E., De Clercq, E., Rao, A., Monforte, A.-M., Chimirri, A. & Neyts, J.
     Anti-enterovirus activity and structure-activity relationship of a series of 2,6-dihalophenyl-substituted 1H,3H-thiazolo[3,4-a]benzimidazoles.
     Biochem. Biophys. Res. Commun., 353: 628-632 (2007).
     


452. Balzarini, J., Schols, D., Van Laethem, K., De Clercq, E., Hocková, D., Masojidkova, M. & Holý, A.
     Pronounced in vitro and in vivo antiretroviral activity of 5-substituted 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidines.
     J. Antimicrob. Chemother., 59, 80-86 (2007).
     


453. Gazivoda, T., Raić-Malić, S., Marjanović, M., Kralj, M., Pavelić, K., Balzarini, J., De Clercq, E. & Mintas, M.
     The novel C-5 aryl, alkenyl and alkynyl substituted uracil derivatives of L-ascorbic acid: synthesis, cytostatic and antiviral activity evaluations.
     Bioorg. Med. Chem., 15: 749-758 (2007).
     



67 publications in the year 2006



454. Chiacchio, U., Saita, M.G., Crispino, L., Gumina, G., Mangiafico, S., Pistarà, V., Romeo, G., Piperno, A. & De Clercq, E.
     Enantioselective synthesis of homocarbocyclic-2’-oxo-3’-azanucleosides.
     Tetrahedron, 62: 1171-1181 (2006).
     


455. De Clercq, E. & Naesens, L.
     In search of effective anti-HHV-6 agents.
     J. Clin. Virol., 37, Suppl. 1: S82-S86 (2006).
     


456. Naesens, L., Bonnafous, P., Agut, H. & De Clercq, E.
     Antiviral activity of diverse classes of broad-acting agents and natural compounds in HHV-6-infected lymphoblasts.
     J. Clin. Virol., 37, Suppl. 1: S69-S75 (2006).
     


457. Rajić, Z., Zorc, B., Raić-Malić, S., Ester, K., Kralj, M., Pavelić, K., Balzarini, J., De Clercq, E. & Mintas, M.
     Hydantoin derivatives of L- and D-amino acids: synthesis and evaluation of their antiviral and antitumoral activity.
     Molecules, 11: 837-848 (2006).
     


458. Yan, R.Z., Liu, X.Y., Xu, W.F., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and anti-HIV evaluation of the novel 2-(m-chlorobenzyl)-4-substituted-7-methyl-1,1,3-trioxo-pyrazolo[4,5-e][1,2,4]thiadiazines.
     Arch. Pharm. Res., 29: 957-962 (2006).
     


459. Selvam, P., Abileshini, B., Alagarsamy, V., Pannecouque, C. & De Clercq, E.
     Synthesis, antiviral and cytotoxicity of some new sulphonamides.
     Indian J. Heterocyclic Chem., 16: 73-74 (2006).
     


460. De Clercq, E.
     From adefovir to AtriplaTM via tenofovir, VireadTM and TruvadaTM.
     Future Virology, 1: 709-715 (2006).
     


461. De Clercq, E.
     Antiviral agents active against influenza A viruses.
     Nature Rev. Drug Discovery, 5: 1015-1025 (2006).
     


462. Liekens, S., Balzarini, J., Hernández, A.I., De Clercq, E., Priego, E.M., Camarasa, M.J. & Pérez-Pérez, M.J.
     Thymidine phosphorylase is noncompetitively inhibited by 5’-O-trityl-inosine (KIN59) and related compounds.
     Nucleosides, Nucleotides, and Nucleic Acids, 25: 975-980 (2006).
     


463. De Clercq, E.
     Editorial to Antiviral Research
     Antiviral Res., 72: 167-170 (2006).
     


464. 
     Synthesis, X-ray crystal structural study, antiviral and cytostatic evaluations of the novel unsaturated acyclic and epoxide nucleoside analogues.
     Bioorg. Med. Chem., 14: 8126-8138 (2006).
     


465. Hořejsí, K., Andrei, G., De Clercq, E., Snoeck, R., Pohl, R. & Holý, A.
     Tricyclic etheno analogs of PMEG and PMEDAP. Synthesis and biological activity.
     Bioorg. Med. Chem., 14: 8057-8065 (2006).
     


466. De Clercq, E.
     Highly potent and selective inhibition of varicella-zoster virus replication by bicyclic furo[2,3-d]pyrimidine nucleoside analogues (BCNAs).
     In: “Herpes Zoster. Recent Aspects of Diagnosis and Control”,Monographs in Virology, vol. 26. G. Gross & H.W. Doerr (eds.), Karger AG, Basel, Switzerland, pp. 131-142 (2006).
     


467. Tušek-Božić, Lj., Cmrečki, V., Balzarini, J. & De Clercq, E.
     Cytotoxicity and antiviral activity of palladium(II) quinolylmethylphosphonate complexes. Synthesis of acetate complexes.
     Lett. Drug Design & Discovery, 3: 528-533 (2006).
     


468. Valks, G.C., McRobbie, G., Lewis, E.A., Hubin, T.J., Hunter, T.M., Sadler, P.J., Pannecouque, C., De Clercq, E. & Archibald, S.J.
     Configurationally-restricted bismacrocyclic CXCR4 receptor antagonists.
     J. Med. Chem., 49: 6162-6165. (2006).
     


469. Coelmont, L., Paeshuyse, J., Windisch, M.P., De Clercq, E., Bartenschlager, R. & Neyts, J.
     Ribavirin antagonizes the in vitro anti-hepatitis C virus activity of 2’-C-methylcytidine, the active component of valopicitabine.
     Antimicrob. Agents Chemother., 50: 3444-3446 (2006).
     


470. Canoa, P., González, M.J., Teijeira, M., Terán, C., Uriarte, E., Pannecouque, C. & De Clercq, E.
     Synthesis and anti-HIV activity of novel cyclopentenyl nucleoside analogues of 8-azapurine.
     Chem. Pharm. Bull., 54: 1418-1420 (2006).
     


471. De Clercq, E.
     The role of tenofovir in the prevention of HIV infections.
     AIDS, 20: 1990-1991 (2006).
     


472. Koszytkowska-Stawińska, M., Sas, W. & De Clercq, E.
     Synthesis of aza-analogues of ganciclovir.
     Tetrahedron, 62: 10325-10331 (2006).
     


473. Setaki, D., Tataridis, D., Stamatiou, G., Kolocouris, A., Foscolos, G.B., Fytas, G., Kolocouris, N., Padalko, E., Neyts, J. & De Clercq, E.
     Synthesis, conformational characteristics and anti-influenza virus A activity of some 2-adamantylsubstituted azacycles.
     Bioorg. Chem., 34: 248-273 (2006).
     


474. Andrei, G., Gammon, D.B., Fiten, P., De Clercq, E., Opdenakker, G., Snoeck, R. & Evans, D.H.
     Cidofovir resistance in vaccinia virus is linked to diminished virulence in mice.
     J. Virol., 80: 9391-9401 (2006).
     


475. Puerstinger, G., Paeshuyse, J., Herdewijn, P., Rozenski, J., De Clercq, E. & Neyts, J.
     Substituted 5-benzyl-2-phenyl-5H-imidazo[4,5-c]pyridines: a new class of pestivirus inhibitors.
     Bioorg. Med. Chem. Lett., 16: 5345-5349 (2006).
     


476. De Clercq, E., Brancale, A;, Vere Hodge, A. & Field, H.J.
     Antiviral chemistry & chemotherapy’s current antiviral agents FactFile 2006 (1st edition).
     Antiviral Chem. Chemother., 17: 113-166 (2006).
     


477. Moukha-chafiq, O., Taha, M.L., Lazrek, H.B, Vasseur, J.-J. & De Clercq, E.
     Synthesis and antiviral activity of some C2-, C4-, and C6-substituted pyrazolo[3,4D]pyrimidine acyclonucleosides with the alkylating chains of ACV, HBG, and iso-DHPG.
     Nucleosides, Nucleotides, and Nucleic Acids, 25: 849-860 (2006).
     


478. Ji, L., Chen, F.-E., Feng, X.Q., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. Synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues.
     Chem. Pharm. Bull. (Tokyo), 54: 1248-1253 (2006).
     


479. Naesens, L., Stephens, C.E., Andrei, G., Loregian, A., De Bolle, L., Snoeck, R., Sowell, J.W. & De Clercq, E.
     Antiviral properties of new arylsulfone derivatives with activity against human betaherpesviruses.
     Antiviral Res., 72: 60-67 (2006).
     


480. Balzarini, J., Keyaerts, E., Vijgen, L., Egberink, H., De Clercq, E., Van Ranst, M., Printsevskaya, S.S.,Olsufyeva, E.N., Solovieva, S.E. & Preobrazhenskaya, M.N.
     Inhibition of feline (FIPV) and human (SARS) coronavirus by semisynthetic derivatives of glycopeptide antibiotics.
     Antiviral Res., 72: 20-33 (2006).
     


481. De Clercq, E.
     Interferon and its inducers - a never-ending story: “old” and “new” data in a new perspective.
     J. Infect. Dis., 194, Suppl. 1: S19-S26 (2006).
     


482. Deng, B.-L., Hartman, T.L., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E. & Cushman, M.
     Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents.
     J. Med. Chem., 49: 5316-5323 (2006).
     


483. Stevens, M., De Clercq, E. & Balzarini, J.
     The regulation of HIV-1 transcription: molecular targets for chemotherapeutic intervention.
     Med. Res. Rev., 26: 595-625 (2006).
     


484. Paeshuyse, J., Coelmont, L., Vliegen, I., Van hemel, J., Vandenkerckhove, J., Peys, E., Sas, B., De Clercq, E. & Neyts, J.
     Hemin potentiates the anti-hepatitis C virus activity of the antimalarial drug artimisinin.
     Biochem. Biophys. Res. Commun., 348: 139-144 (2006).
     


485. Naesens, L., De Bolle, L. & De Clercq, E.
     Therapeutic approaches to HHV-6 infection.
     In: Human Herpesvirus-6. General Virology, Epidemiology and Clinical Pathology. Krueger, G. & Ablashi, D.V., eds. Perspectives in Medical Virology, vol. 12. Elsevier, Amsterdam, pp. 291-301 (2006).
     


486. Al-Masoudi, N.A., Al-Soud, Y.A., Kalogerakis, A., Pannecouque, C. & De Clercq, E.
     Nitroimidazoles. Part 2. Synthesis, antiviral and antitumor activity of new 4-nitroimidazoles.
     Chemistry & Biodiversity, 3: 515-526 (2006).
     


487. Janeba, Z., Balzarini, J., Andrei, G., Snoeck, R., De Clercq, E. & Robins, M.J.
     Synthesis and biological evaluation of 5-(alkyn-1-yl)-1-(p-toluenesulfonyl)uracil derivatives.
     Can. J. Chem., 84: 580-586 (2006).
     


488. De Clercq, E.
     Hope and hype. Book review on “Interferon. The Science and Selling of a Miracle Drug”, Pieters, T., Ed., Routledge, Taylor & Francis Group, 2005, 264 pp.
     Nature Medicine, 12: 727 (2006).
     


489. Torii, T., Onishi, T., Izawa, K., Maruyama, T., Demizu, Y., Neyts, J. & De Clercq, E.
     Synthesis of 6-arylthio analogs of 2’,3’-dideoxy-3’-fluoroguanosine and their effect against hepatitis B virus replication.
     Nucleosides, Nucleotides, Nucleic Acids, 25: 655-665 (2006).
     


490. Lenaerts, L., Daelemans, D., Geukens, N., De Clercq E. & Naesens, L.
     Mouse adenovirus type 1 attachment is not mediated by the Coxsackie-adenovirus receptor.
     FEBS Lett., 580: 3937-3942 (2006).
     


491. Lebeau, I., Andrei, G., Dal Pozzo, F., Beadle, J.R., Hostetler, K.Y., De Clercq, E., van den Oord, J. & Snoeck, R.
     Activities of alkoxyalkyl esters of cidofovir (CDV), cyclic CDV, and (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine against orthopoxviruses in cell monolayers and in organotypic cultures.
     Antimicrob. Agents Chemother., 50: 2525-2529 (2006).
     


492. de Castro, S., García-Aparicio, C., Van Laethem, K., Gago, F., Lobatón, E., De Clercq, E., Balzarini, J., Camarasa, M.-J. & Velázquez, S.
     Discovery of TSAO derivatives with an unusual HIV-1 activity/resistance profile.
     Antiviral Res., 71: 15-23 (2006).
     


493. Jha, A., Zhao, J., Cameron, T.S., De Clercq, E., Balzarini, J., Manavathu, E.K. & Stables, J.P.
     Design, synthesis and biological evaluation of novel curcumin analogs as anti-neoplastic agents.
     Lett. Drug Design & Discovery, 3: 304-310 (2006).
     


494. De Clercq, E.
     Influenza virus inhibitors available for the chemotherapy and/or chemoprophylaxis of influenza virus infections.
     Verh. K. Acad. Geneesk. Belg., 68: 121-137 (2006).
     


495. Das, U., Gul, H.I., Alcorn, J., Shrivastav, A., George, T., Sharma, R.K., Nienaber, K.H., De Clercq, E., Balzarini, J., Kawase, M., Kan, N., Tanaka, T., Tani, S., Werbovetz, K.A., Yakovich, A.J, Manavathu, E.K., Stables, J.P. & Dimmock, J.R.
     Cytotoxic 5-aryl-1-(4-nitrophenyl)-3-oxo-1,4-pentadienes mounted on alicyclic scaffolds.
     Eur. J. Med. Chem., 41: 577-585 (2006).
     


496. Grison, C., Joliez, S., De Clercq, E. & Coutrot, P.
     Monoglycosyl, diglycosyl, and dinucleoside methylenediphosphonates: direct synthesis and antiviral activity.
     Carbohydrate Res., 341: 1117-1129 (2006).
     


497. Biot, C., Daher, W., Chavain, N., Fandeur, T., Khalife, J., Dive, D. & De Clercq, E.
     Design and synthesis of hydroxyferroquine derivatives with antimalarial and antiviral activities.
     J. Med. Chem., 49: 2845-2849 (2006).
     


498. Küçükgüzel, G., Kocatepe, A., De Clercq, E., Sahin, F. & Güllüce, M.
     Synthesis and biological activity of 4-thiazolidinones, thiosemicarbazides derived from diflunisal hydrazide.
     Eur. J. Med. Chem., 41: 353-359 (2006).
     


499. Tabarrini, O., Manfroni, G., Fravolini, A., Cecchetti, V., Sabatini, S., De Clercq, E., Rozenski, J., Canard, B., Dutartre, H., Paeshuyse, J. & Neyts, J.
     Synthesis and anti-BVDV activity of acridones as new potential antiviral agents.
     J. Med. Chem., 49: 2621-2627 (2006).
     


500. De Clercq, E.
     Potential antivirals and antiviral strategies against SARS coronavirus infections.
     Expert Rev. Anti Infect. Ther., 4: 291-302 (2006).
     


501. Leyssen, P., De Clercq, E. & Neyts, J.
     The anti-yellow fever virus activity of ribavirin is independent of error-prone replication.
     Mol. Pharmacol., 69: 1461-1467 (2006).
     


502. Ostrowski, T., Golankiewicz, B., De Clercq, E. & Balzarini, J.
     Synthesis and biological activity of tricyclic analogues of 9-{[cis-1’,2’-bis(hydroxymethyl)cycloprop-1’-yl]methyl}guanine.
     Bioorg. Med. Chem., 14: 3535-3542 (2006)
     


503. Zoidis, G., Fytas, C., Papanastasiou, I., Foscolos, G.B., Fytas, G., Padalko, E., De Clercq, E., Naesens, L., Neyts, J. & Kolocouris, N.
     Heterocyclic rimantadine analogues with antiviral activity.
     Bioorg. Med. Chem., 14: 3341-3348 (2006).
     


504. Farghaly, A.-R., De Clercq, E. & El-Kashef, H.
     Synthesis and antiviral activity of novel [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, [1,2,4]triazole[3,4-b][1,3,4]thiadiazines and [1,2,4]triazolo[3,4-b][1,2,3]thiadiazepines.
     ARKIVOC, 137-151 (2006).
     


505. Paeshuyse, J., Kaul, A., De Clercq, E., Rosenwirth, B., Dumont, J.-M., Scalfaro, P., Bartenschlager, B. & Neyts, J.
     The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro.
     Hepatology, 43: 761-770 (2006).
     


506. Stevens, M., Pannecouque, C., De Clercq, E. & Balzarini, J.
     Pyridine N-oxide derivatives inhibit viral transactivation by interfering with NF-kB binding.
     Biochem. Pharmacol., 71: 1122-1135 (2006).
     


507. Maruyama, T., Kozai, S., Demizu, Y., Witvrouw, M., Pannecouque, C., Balzarini, J., Snoeck, R., Andrei, G. & De Clercq, E.
     Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives.
     Chem. Pharm. Bull., 54: 325-333 (2006).
     


508. Balzarini, J., Keyaerts, E., Vijgen, L., Vandermeer, F., Stevens, M., De Clercq, E., Egberink, H. & Van Ranst, M.
     Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture.
     J. Antimicrob. Chemother., 57: 472-481 (2006).
     


509. An, J., Liu, J.-Z., Wu, C.-F., Li, J., Dai, L., Van Damme, E., Balzarini, J., De Clercq, E., Chen, F. & Bao, J.-K.
     Anti-HIV I/II activity and molecular cloning of a novel mannose-sialic acid-binding lectin from rhizome of Polygonatum cyrtonema hua.
     Acta Biochim. Biophys. Sinica, 38: 70-78 (2006).
     


510. Deng, B.-L., Cullen, M.D., Zhou, Z., Hartman, T.L., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E., Fanwick, P.E. & Cushman, M.
     Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole ring.
     Bioorg. Med. Chem., 14: 2366-2374 (2006).
     


511. Guillerm, G., Muzard, M., Glapski, C., Pilard, S. & De Clercq, E.
     Inactivation of S-adenosyl-L-homocysteine hydrolase by 6’-cyano-5’,6’-didehydro-6’-deoxyhomoadenosine and 6’-chloro-6’-cyano-5’,6’-didehydro-6’-deoxyhomoadenosine. Antiviral and cytotoxic effects.
     J. Med. Chem., 49: 1223-1226 (2006).
     


512. Stittelaar, K.J., Neyts, J., Naesens, L., van Amerongen, G., van Lavieren, R.F., Holý, A., De Clercq, E., Niesters, H.G.M., Fries, E., Maas, C., Mulder, P.G.H, van der Zeijst, B.A.M. & Osterhaus, A.D.M.E.
     Antiviral treatment is more effective than smallpox vaccination upon lethal monkeypox virus infection.
     Nature, 439 : 745-748 (2006).
     


513. Rescifina, A., Chiacchio, U., Corsaro, A., De Clercq, E., Iannazzo, D., Mastino, A., Piperno, A., Romeo, G., Romeo, R. & Valveri, V.
     Synthesis and biological activity of isoxazolidinyl polycyclic aromatic hydrocarbons: potential DNA intercalators.
     J. Med. Chem., 49: 709-715 (2006).
     


514. De Clercq, E. & Field, H.J.
     Antiviral prodrugs – the development of successful prodrug strategies for antiviral chemotherapy.
     Brit. J. Pharmacol., 147: 1-11 (2006).
     


515. González-Díaz, H., Vina, D, Santana, L., De Clercq, E. & Uriarte, E.
     Stochastic entropy QSAR for the in silico discovery of anticancer compounds: prediction, synthesis, and in vitro assay of new purine carbanucleosides.
     Bioorg. Med. Chem., 14: 1095-1107 (2006).
     


516. Robins, M.J., Miranda, K., Rajwanshi, V.K., Peterson, M.A., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis and biological evaluation of 6-(alkyn-1-yl)furo[2,3-d]pyrimidin-2(3H)-one base and nucleoside derivatives.
     J. Med. Chem., 49: 391-398 (2006).
     


517. Barral, K., Balzarini, J., Neyts, J., De Clercq, E., Hider, R.C. & Camplo, M.
     Synthesis and antiviral evaluation of cyclic and acyclic 2-methyl-3-hydroxy-4-pyridinone nucleoside derivatives.
     J. Med. Chem., 49: 43-50 (2006).
     


518. Terzioğlu, N., Karali, N., Gürsoy, A., Pannecouque, C., Leyssen, P., Paeshuyse, J., Neyts, J. & De Clercq, E.
     Synthesis and primary antiviral activity evaluation of 3-hydrazono-5-nitro-2-indolino derivatives.
     ARKIVOC, 109-118 (2006).
     


519. De Clercq, E.
     A guided tour through the antiviral drug field.
     Future Virology, 1: 19-35 (2006).
     


520. Paeshuyse, J., Leyssen, P., Mabery, E., Boddeker, N., Vrancken, R., Froeyen, M., Ansari, I.H., Dutartre, H., Rozenski, J., Gil, L.H.V.G., Letellier, C., Lanford, R., Canard, B., Koenen, F., Kerkhofs, P., Donis, R.O., Herdewijn, P., Watson, J., De Clercq, E., Pürstinger, G. & Neyts, J.
     A novel, highly selective inhibitor of pestivirus replication that targets the viral RNA-dependent RNA polymerase.
     J. Virol., 80: 149-160 (2006).
     



76 publications in the year 2005



521. Ramajayam, R., Giridhar, R., Yadav, M.R., De Clercq, E., Pannecouque, C. & Prajapati, D.G.
     Identification of novel non-nucleoside reverse transcriptase inhibitors using fragment-based lead generation.
     Med. Chem. Res., 14: 475-487 (2005).
     


522. Fanourgiakis, P., Georgala, A., Vekemans, M., Triffet, A., De Bruyn, J.-M., Duchateau, V., Martiat, P., De Clercq, E., Snoeck, R., Wollants, E., Rector, A., Van Ranst, M. & Aoun, M.
     Intravesicular instillation of cidofovir in the treatment of hemorrhagic cystitis caused by adenovirus type 11 in a bone marrow transplant recipient.
     Clin. Infect. Dis., 40: 199-201 (2005).
     


523. Mallants, R., Van Oosterwyck, K., Van Vaeck, L., Mols, R., De Clercq, E. & Augustijns, P.
     Multipledrug resistance-associated protein 2 (MRP-2) affects hepatobiliary elimination but not the intestinal disposition of tenofovir disoproxil fumarate and its metabolites.
     Xenobiotica, 35: 1055-1066 (2005).
     


524. De Clercq, E.
     John Montgomery’s legacy: carbocyclic adenosine analogues as SAH hydrolase inhibitors with broad-spectrum antiviral activity
     Nucleosides, Nucleotides & Nucleic Acids, 24: 1395-1415 (2005).
     


525. Zhou, L., Amer, A., Korn, M., Burda, R., Balzarini, J., De Clercq, E., Kern, E.R. & Torrence, P.F.
     Synthesis and antiviral activities of 1,2,3-triazole functionalized thymidines: 1,3-dipolar cycloaddition for efficient regioselective diversity generation.
     Antiviral Chem. Chemother., 16: 375-383 (2005).
     


526. Dal Pozzo, F., Andrei, G., Holý, A., Van Den Oord, J., Scagliarini, A., De Clercq, E. & Snoeck, R.
     Activity of acyclic nucleoside phosphonates against orf virus in human and ovine cell monolayers and organotypic ovine raft cultures.
     Antimicrob. Agents Chemother., 49: 4843-4852 (2005).
     


527. Selvam, P., Girija, K., Nagarajan, G. & De Clercq, E.
     Synthesis, antibacterial and antiHIV activities of 3-[5-amino-6-(2,3-dichloro-phenyl)-[1,2,4]triazin-3-yl]-6,8-dibromo-2-substituted-3H-quinazolin-4-one.
     Indian J. Pharm. Sci., 484-487 (2005).
     


528. De Clercq, E.
     Zoektocht naar nieuwe antivirale middelen aan het Rega Instituut.
     Azimuz, 1: 4-13 (2005).
     


529. De Clercq, E.
     Interferon: ten stories in one. A short review of some of the highlights in the history of an almost quinquagenarian
     Acta Microbiol. Immunol. Hung., 52: 273-289 (2005).
     


530. Bonache, M.-C., Chamorro, C., Velázquez, S., De Clercq, E., Balzarini, J., Barrios, F.R., Gago, F., Camarasa, M.-J. & San-Félix, A.
     Improving the antiviral efficacy and selectivity of HIV-1 reverse transcriptase inhibitor TSAO-T by the introduction of functional groups at the N-3 position.
     J. Med. Chem., 48: 6653-6660 (2005).
     


531. De Clercq, E. & Holý, A.
     Acyclic nucleoside phosphonates: a key class of antiviral drugs.
     Nature Rev. Drug Discovery, 4: 928-940 (2005).
     


532. Rawal, R., Prabhakar, Y.S., Katti, S.B. & De Clercq, E.
     2-(Aryl)-3-furan-2-ylmethyl-thiazolidin-4-ones as selective HIV-RT inhibitors.
     Bioorg. Med. Chem., 13: 6771-6776 (2005).
     


533. Lenaerts, L., Verbeken, E., De Clercq, E. & Naesens, L.
     Mouse adenovirus type 1 infection in SCID mice: an experimental model for antiviral therapy of systemic adenovirus infections.
     Antimicrob. Agents Chemother., 49: 4689-4699 (2005).
     


534. Andrei, G., van den Oord, J., Fiten, P., Opdenakker, G., De Wolf-Peeters, C., De Clercq, E. & Snoeck, R.
     Organotypic epithelial raft cultures as a model for evaluating compounds against alphaherpesviruses.
     Antimicrob. Agents Chemother., 49: 4671-4680 (2005).
     


535. Stevens, M., Balzarini, J., Tabarrini, O., Andrei, G., Snoeck, R., Cecchetti, V., Fravolini, A., De Clercq, E. & Pannecouque, C.
     Cell-dependent interference of a series of new 6-aminoquinolone derivatives with viral (HIV/CMV) transactivation.
     J. Antimicrob. Chemother., 56: 847-855 (2005).
     


536. Scagliarini, A., Dal Pozzo, F., Gallina, L., Guercio, A., De Clercq, E., Snoeck, R. & Andrei, G.
     Ovine skin organotypic cultures applied to the ex vivo study of orf virus infection.
     Vet. Res. Comm., 29, Suppl. 2: 245-247 (2005).
     


537. Kelleher, M.R., McGuigan, C., Bidet, O., Carangio, A., Weldon, H., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     The journey towards elucidating the anti-HCMV activity of alkylated bicyclic furano pyrimidines.
     Proceedings of the XVIth International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Minneapolis, Minnesota, USA, 12-16 September 2004.
     Nucleosides, Nucleotides & Nucleic Acids, 24: 643-645 (2005).
     


538. Kelleher, M.R., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis and biological evaluation of N- and O-alkylated bicyclic furanopyrimidines as non-nucleosidic inhibitors of human cytomegalovirus.
     Proceedings of the XVIth International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Minneapolis, Minnesota, USA, 12-16 September 2004.
     Nucleosides, Nucleotides & Nucleic Acids, 24: 639-641 (2005).
     


539. Goslinski, T., Januszczyk, P., Wenska, G., Golankiewicz, B., De Clercq, E. & Balzarini, J.
     Synthesis and fluorescent properties of the tricyclic analogues of acyclovir linked with nitrogen heterocyclic units.
     Proceedings of the XVIth International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Minneapolis, Minnesota, USA, 12-16 September 2004.
     Nucleosides, Nucleotides & Nucleic Acids, 24: 571-575 (2005).
     


540. De Clercq, E., Andrei, G., Balzarini, J., Leyssen, P., Naesens, L., Neyts, J., Pannecouque, C., Snoeck, R., Ying, C., Hocková, D. & Holý, A.
     Antiviral potential of a new generation of acyclic nucleoside phosphonates, the 6-[2-(phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines.
     Proceedings of the XVIth International Round Table on Nucleosides, Nucleotides and Nucleic Acids, Minneapolis, Minnesota, USA, 12-16 September 2004.
     Nucleosides, Nucleotides & Nucleic Acids, 24: 331-341 (2005).
     


541. Sun, G.-F., Kuang, Y.-Y., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Non-nucleoside HIV reverse transcriptase inhibitors, Part 6[1]: Synthesis and anti-HIV activity of novel 2-[(arylcarbonylmethyl)thio]-6-arylthio DABO analogues.
     Arch. Pharm. Chem. Life Sci., 338: 457-461 (2005).
     


542. Prekupec, S., Makuc, D., Plavec, J., Kraljevíc, S., Kralj, M., Pavelíc, K., Andrei, G., Snoeck, R., Balzarini, J., De Clercq, E., Raic-Malíc, S. & Mintas, M.
     Antiviral and cytostatic evaluation of the novel 6-acyclic chain substituted thymine derivatives.
     Antiviral Chem. Chemother., 26: 327-338 (2005).
     


543. Yang, G., Pevear, D.C., Davies, M.H., Collett, M.S., Bailey, T., Rippen, S., Barone, L., Burns, C., Rhodes, G., Tohan, S., Huggins, J.W., Baker, R.O., Buller, R.L.M., Touchette, E., Waller, K., Schriewer, J., Neyts, J., De Clercq, E., Jones, K., Hruby, D. & Jordan, R.
     An orally bioavailable antipoxvirus compound (ST-246) inhibits extracellular virus formation and protects mice from lethal orthopoxvirus challenge.
     Antimicrob. Agents Chemother., 79: 13139-13149 (2005).
     


544. Deng, B.-L., Hartman, T.L., Buckheit, R.W. Jr., Pannecouque, C., De Clercq, E., Fanwick, P.E. & Cushman, M.
     Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors.
     J. Med. Chem., 48: 6140-6155 (2005).
     


545. De Clercq, E.
     Recent highlights in the development of new antiviral drugs.
     Curr. Opin. Microbiol., 8: 552-560 (2005).
     


546. Otshudi, A.L., Apers, S., Pieters, L., Claeys, M., Pannecouque, C., De Clercq, E., Van Zeebroeck, A., Lauwers, S., Frédérich, M. & Foriers, A.
     Biologically active bisbenzylisoquinoline alkaloids from the root bark of Epinetrum villosum.
     J. Ethnopharmacol., 102: 89-94 (2005).
     


547. Auwerx, J., Rodríguez-Barrios, F., Ceccherini-Silberstein, F., San-Félix, A., Velázquez, S., De Clercq, E., Camarasa, M.-J., Perno, C.-F., Gago, F. & Balzarini, J.
     The role of Thr139 in the human immunodeficiency virus type 1 reverse transcriptase sensitivity to (+)-calanolide A.
     Mol. Pharmacol., 68: 652-659 (2005).
     


548. De Clercq, E.
     Potential clinical applications of the CXCR4 antagonist bicyclam AMD3100.
     Mini-Reviews in Medicinal Chemistry, 5: 805-824 (2005).
     


549. Hantson, A., Fikkert, V., Van Remoortel, B., Pannecouque, C., Cherepanov, P., Matthews, B., Holan, G., De Clercq, E., Vandamme, A.-M., Debyser, Z. & Witvrouw, M.
     Mutations in both env and gag genes are required for HIV-1 resistance to the polysulfonic dendrimer SPL2923, as corroborated by chimeric virus technology.
     Antiviral Chem. Chemother., 16: 253-266 (2005).
     


550. De Clercq, E.
     Antiviral drug targets and strategies for emerging viral diseases and bioterrorism threats”.
     In: “Antiviral Drug Discovery for Emerging Diseases and Bioterrorism”, Torrence, P.F. ed. John-Wiley & Sons, Inc., Hoboken, New Jersey, USA, pp. 83-113 (2005).
     


551. Romagnoli, R., Baraldi, P.G., Jung, M.K., Iaconinoto, M.A., Carrion, M.D., Remusat, V., Preti, D., Tabrizi, M.A., Francesca, F., De Clercq, E., Balzarini, J. & Hamel, E.
     Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
     Bioorg. Med. Chem. Lett., 15: 4048-4052 (2005).
     


552. De Clercq, E.
     Antiviral drug discovery and development: where chemistry meets with medicine.
     Antiviral Res., 67: 56-75 (2005).
     


553. Tsotinis, A., Vlachou, M., Eleutheriades, A., Garratt, P.J., Ibbett, A.J., Ng, Y.-F., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Aromatic polycationic molecules with restricted conformations: an alternative approach to antiherpes agents.
     Lett. Drug Design & Discovery, 2: 424-427 (2005).
     


554. Sun, G.-F., Chen, X.-X., Chen, F.-E., Wang, Y.-P., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Nonnucleoside HIV-1 reverse-transcriptase inhibitors, Part 5. Synthesis and anti-HIV-1 activity of novel 6-naphthylthio HEPT analogues.
     Chem. Pharm. Bull., 53: 886-892 (2005).
     


555. He, Y., Kuang, Y., Chen, F., Wang, S., Ji, L., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Nonnucleoside HIV-1 reverse transcriptase inhibitors, Part 4[1]. Synthesis and anti-HIV activity of N-1-β-carbonyl-6-naphthylmethyl analogues of HEPT.
     Monatshefte für Chemie, 136: 1233-1245 (2005).
     


556. Janeba, Z., Balzarini, J., Andrei, G., Snoeck, R., De Clercq, E. & Robins, M.J.
     Synthesis and biological evaluation of acyclic 3-[(2-hydroxyethoxy)methyl] analogues of antiviral furo- and pyrrolo[2,3-d]pyrimidine nucleosides.
     J. Med. Chem., 48: 4690-4696 (2005).
     


557. Hatse, S., Princen, K., De Clercq, E., Rosenkilde, M.M., Schwartz, T.W., Hernandez-Abad, P.E., Skerlj, R.T., Bridger, G.J. & Schols, D.
     AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor.
     Biochem. Pharmacol., 70: 752-761 (2005).
     


558. Girija, K., Selvam, P., Nagarajan, R., De Clercq, E. & Gopal, V.
     Synthesis and cytostatic activity of some 3-[5-amino-6-(2,3-dichlorophenyl)-[1,2,4]triazin-3-yl]-6,8-dibromo-2-substituted-3H-quinazolin-4-ones.
     Indian J. Heterocyclic Chem., 14: 255-256 (2005).
     


559. Luoni, G., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus: the effect of branching in the p-alkylphenyl side chain.
     Bioorg. Med. Chem. Lett., 15: 3791-3796 (2005).
     


560. De Clercq, E.
     Antiviral drugs: triphosphates of nucleoside analogues active as antiviral drugs
     In: “Nucleoside Triphosphate and their Analogs: Chemistry, Biotechnology and Biological Applications”, M. Vaghefi (ed.), Taylor & Francis, Boca Raton, FL, USA, pp. 329-341 (2005).
     


561. Rawal, R.K., Solomon, V.R., Prabhakar, Y.S., Katti, S.B. & De Clercq, E.
     Synthesis and QSAR studies on thiazolidinones as anti-HIV agents.
     Combinatorial Chemistry & High Through-put Screening, 8: 439-443 (2005).
     


562. Nguyen Van Nhien, A., Tomassi, C., Len, C., Marco-Contelles, J.L., Balzarini, J., Pannecouque, C., De Clercq, E. & Postel, D.
     First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication.
     J. Med. Chem., 48: 4276-4284 (2005).
     


563. De Clercq, E. & Herdewijn, P.
     Strategies in the design of antiviral drugs.
     In: “Drug Discovery Handbook”, S. Gad (ed.). John Wiley & Sons, New York, pp. 1135-1190 (2005).
     


564. De Clercq, E.
     Anti-HIV chemotherapy: current state of the art.
     Proceedings of the Second International Symposium on Current Trends in Drug Discovery and Research (CTDDR), Central Drug Research Institute, Lucknow, India.
     Med. Chem. Res., 13: 439-478 (2005).
     


565. Balzarini, J., Auwerx, J., Rodríguez-Barrios, F., Chedad, A., Farkas, V., Ceccherini-Silberstein, F., García-Aparicio, C., Velázquez, S., De Clercq, E., Perno, C.-F., Camarasa, M.-J. & Gago, F.
     The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors.
     Mol. Pharmacol., 68: 49-60 (2005).
     


566. Witvrouw, M., Fikkert, V., Hantson, A., Pannecouque, C., O’Keefe, B.R., McMahon, J., Stamatatos, L., De Clercq, E. & Bolmstedt, A..
     Resistance of human immunodeficiency virus type 1 to the high-mannose binding agents Cyanovirin N and Concanavalin A.
     J. Virol., 79: 7777-7784 (2005).
     


567. De Clercq, E.
     Emerging anti-HIV drugs.
     Expert Opin. Emerging Drugs, 10: 241-274 (2005).
     


568. Printsevskaya, S.S., Solovieva, S.E., Olsufyeva, E.N., Mirchink, E.P., Isakova, E.B., De Clercq, E., Balzarini, J. & Preobrazhenskaya, M.N.
     Structure-activity relationship studies of a series of antiviral and antibacterial aglycon derivatives of the glycopeptide antibiotics vancomycin, eremomycin and dechloroeremomycin.
     J. Med. Chem., 48: 3885-3890 (2005).
     


569. McGuigan, C., Harris, S.A., Daluge, S.M., Gudmundsson, K.S., McLean, E.W., Burnette, T.C., Marr, H., Hazen, R., Condreay, L.D., Johnson, L., De Clercq, E. & Balzarini, J.
     Application of phosphoramidate pronucleotide technology to abacavir leads to a significant enhancement of antiviral potency.
     J. Med. Chem., 48: 3504-3515 (2005).
     


570. van Griensven, J., De Clercq, E. & Debyser, Z.
     Hematopoietic stem cell-based gene therapy against HIV infection: promises and caveats.
     AIDS Rev., 7: 44-55 (2005).
     


571. Barreca, M.L., Rao, A., De Luca, L., Zappalà, M., Monforte, A.-M., Maga, G., Pannecouque, C., Balzarini, J., De Clercq, E., Chimirri, A. & Monforte, P.
     Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
     J. Med. Chem., 48: 3433-3437 (2005).
     


572. Prekupec, S., Kalokira, B., Grdisa, M., Pavelić, K., De Clercq, E., Mintas, M. & Raić-Malić, S.
     Synthesis and comparative cytostatic activity of the new N-7 acyclic purine nucleoside analogues with natural N-9 regioisomers.
     Heterocycles, 65: 787-796 (2005).
     


573. Daelemans, D., Pannecouque, C., Pavlakis, G.N., Tabarrini, O. & De Clercq, E.
     A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors.
     Mol. Pharmacol., 67: 1574-1580 (2005).
     


574. Balzarini, J., Van Laethem, K., Hatse, S., Froeyen, M., Van Damme, E., Bolmstedt, A., Peumans, W., De Clercq, E. & Schols, D.
     Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis.
     Mol. Pharmacol., 67: 1556-1565 (2005).
     


575. Auwerx, J., Van Nieuwenhove, J., Rodríguez-Barrios, F., de Castro, S., Velázquez, S., Ceccherini-Silberstein F, De Clercq, E., Camarasa, M.-J., Perno, C.-F., Gago, F. & Balzarini, J.
     The N137 and P140 amino acids in the p51 and the P95 amino acid in the p66 subunit of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase are instrumental to maintain catalytic activity and to design new classes of anti-HIV-1 drugs.
     FEBS Lett., 579: 2294-2300 (2005).
     


576. Andrei, G., Balzarini, J., Fiten, P., De Clercq, E., Opdenakker, G. & Snoeck, R.
     Characterization of herpes simplex virus type 1 thymidine kinase mutants selected under single round of high-dose brivudin.
     J. Virol., 79: 5863-5869 (2005).
     


577. Selvam, P., Rajasekaran, A., Dharamsi, A., Ahmed, K.L., Musthafa, S.M., Poornima, K., Pournami, K.A., Murugesh, N., Chandramohan, M. & De Clerccq, E.
     Synthesis and antiviral activity of some novel isatin derivatives.
     Asian J. Chem., 17: 443-448 (2005).
     


578. Gerona-Navarro, G., Pérez de Vega, M.J., García-López, M.T., Andrei, G., Snoeck, R., De Clercq, E., Balzarini, J. & González-Muniz, R.
     From 1-acyl--lactams human cytomegalovirus protease inhibitors to 1-benzyloxycarbonylazetidines with improved antiviral activity. A straightforward approach to convert covalent to noncovalent inhibitors.
     J. Med. Chem., 48: 2612-2621 (2005).
     


579. De Clercq, E.
     New approaches toward anti-HIV chemotherapy.
     J. Med. Chem, 48: 1297-1313 (2005).
     


580. Wu, T., Froeyen, M., Kempeneers, V., Pannecouque, C., Wang, J., Busson, R., De Clercq, E. & Herdewijn, P.
     Deoxythreosyl phosphonate nucleosides as selective anti-HIV agents.
     J. Am. Chem. Soc., 127: 5056-5065 (2005).
     


581. de Castro, S., Lobatón, E., Pérez-Pérez, M.-J., San-Félix, A., Cordeiro, A., Andrei, G., Snoeck, R., De Clercq, E., Balzarini, J., Camarasa, M.-J. & Velázquez, S.
     Novel [2’,5’-bis-O-(tert-butyldimethylsilyl)-β-D-ribofuranosyl]-3’-spiro-5”-(4”-amino-1”,2”-oxathiole-2”,2”-dioxide) derivatives with anti-HIV-1 and anti-human-cytomegalovirus activity.
     J. Med. Chem., 48: 1158-1168 (2005).
     


582. González-Díaz, H., Cruz-Monteagudo, M., Vina, D., Santana, L., Uriarte, E. J. & De Clercq, E.
     QSAR for anti-RNA-virus activity, synthesis, and assay of anti-RSV carbonucleosides given a unified representation of spectral moments, quadratic, and topologic indices.
     Bioorg. Med. Chem. Lett., 15: 1651-1657 (2005).
     


583. Barbarić, M, Ursić, S., Pilepić, V., Zorc, B., Hergold-Brundić, A., Nagl, A., Grdisa, M., Pavelić, K., Snoeck, R., Andrei, J., Balzarini, J., De Clercq, E. & Mintas, M.
     Synthesis, X-ray crystal structure study, and cytostatic and antiviral evaluation of the novel cycloalkyl-N-aryl-hydroxamic acids.
     J. Med. Chem., 48: 884-887 (2005).
     


584. Ying, C., Holý, A., Hocková, D, Havlas, Z., De Clercq, E. & Neyts, J.
     Novel acyclic nucleoside phosphonate analogues with potent anti-hepatitis B virus activities.
     Antimicrob. Agents Chemother., 49: 1177-1180 (2005).
     


585. Andrei, G., Sienaert, R., McGuigan, C., De Clercq, E., Balzarini, J. & Snoeck, R.
     Susceptibilities of several clinical varicella-zoster virus (VZV) isolates and drug-resistant VZV strains to bicyclic furano pyrimidine nucleosides.
     Antimicrob. Agents Chemother., 49: 1081-1086 (2005).
     


586. Naesens, L., Lenaerts, L., Andrei, G., Snoeck, R., Van Beers, D., Holý, A., Balzarini, J. & De Clercq, E.
     Antiadenovirus activities of several classes of nucleoside and nucleotide analogues.
     Antimicrob. Agents Chemother., 49: 1010-1016 (2005).
     


587. Ostrowski, T., Golankiewicz, B., De Clercq, E. & Balzarini, J.
     Fluorosubstitution and 7-alkylation as prospective modifications of biologically active 6-aryl derivatives of tricyclic acyclovir and ganciclovir analogues.
     Bioorg. Med. Chem., 13: 2089-2096 (2005).
     


588. Opačič, N., Barbarić, M., Zorc, B., Cetina, M., Nagl, A., Frković, D., Kralj, M., Pavelić, K., Balzarini, J., Andrei, G., Snoeck, R., De Clercq, Raić-Malić, S. & Mintas, M.
     The novel L- and D-amino acid derivatives of hydroxyurea and hydantoins: synthesis, X-ray crystal structure study, and cytostatic and antiviral activity evaluations.
     J. Med. Chem., 48: 475-482 (2005).
     


589. Barral, K., Courcambeck, J., Pèpe, G., Balzarini, J., Neyts, J., De Clercq, E. & Camplo, M.
     Synthesis and antiviral evaluation of cis-substituted cyclohexenyl and cyclohexanyl nucleosides.
     J. Med. Chem., 48: 450-456 (2005).
     


590. Balzarini, J., Stevens, M., De Clercq, E., Schols, D. & Pannecouque, C.
     Pyridine N-oxide derivatives: unusual anti-HIV compounds with multiple mechanisms of antiviral action.
     J. Antimicrob. Chemother., 55: 135-138 (2005).
     


591. De Bolle, L., Naesens, L. & De Clercq, E.
     Update on human herpesvirus 6 biology, clinical features, and therapy.
     Clin. Microbiol. Rev., 18: 217-245 (2005).
     


592. Leyssen, P., Balzarini, J., De Clercq, E. & Neyts, J.
     The predominant mechanism by which ribavirin exerts its antiviral activity in vitro against flaviviruses and paramyxoviruses is mediated by inhibition of IMP dehydrogenase.
     J. Virol., 79: 1943-1947 (2005).
     


593. de Bilderling, G., Bodart, E., Lawson, G., Tuerlinckx, D., Remacle, M., Naesens, L., De Clercq, E. & Snoeck, R.
     Successful use of intralesional and intravenous cidofovir in association with indole-3-carbinol in an 8-year-old girl with pulmonary papillomatosis.
     J. Med. Virol., 75: 332-335 (2005).
     


594. De Bolle, L., Van Loon, J., De Clercq, E. & Naesens, L.
     Quantitative analysis of human herpesvirus 6 cell tropism.
     J. Med. Virol., 75: 76-85 (2005).
     


595. Gazivoda, T., Plevnik, M., Plavec, J., Kraljević, S., Kralj, M., Pavelić, K., Balzarini, J., De Clercq, E. Mintas, M. & Raic-Malić, S.
     The novel pyrimidine and purine derivatives of L-ascorbic acid: synthesis, one- and two-dimensional 1H and 13C NMR study, cytostatic and antiviral evaluation.
     Bioorg. Med. Chem., 13: 131-139 (2005).
     


596. De Clercq, E.
     (E)-5-(2-Bromovinyl)-2’-deoxyuridine (BVDU)
     Med. Res. Rev., 25: 1-20 (2005).
     



85 publications in the year 2004



597. De Clercq, E.
     Profiles of prototype antiviral agents interfering with the initial stages of HIV infections.
     In: “Drug Discovery Strategies and Methods”, A. Makriyannis & D. Biegel (eds.). Marcel Dekker, Inc., New York, Basel, pp. 309-336 (2004).
     


598. Rosen, T.C., De Clercq, E., Balzarini, J. & Haufe, G.
     Synthesis and antiviral activity of monofluorinated cyclopropanoid nucleosides.
     Org. Biomol. Chem., 2: 229-237 (2004).
     


599. Selvam, P., Chennama, B., Murugesh, N., Chandramohan, M. & De Clercq, E.
     Synthesis and antiviral activity of some novel 2-substituted, 3-(6-ethyl, 4-amino, 5-(4-chlorophenyl)-pyrimidin-2-yl)quinazolin-4(3H)-ones.
     Int. J. Chem. Sci., 2: 627-631 (2004).
     


600. Sinha, S., Srivastava, R., De Clercq, E. & Singh, R.K.
     Synthesis and antiviral properties of arabino and ribonucleosides of 1,3-dideazaadenine, 4-nitro-1,3-dideazapurine and diketopiperazine.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 1815-1824 (2004).
     


601. Luoni, G., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus modified on the sugar moiety: 3’ and 5’ derivatives.
     Antiviral Chem. Chemother., 15: 333-341 (2004).
     


602. Bidet, O., McGuigan, C., Snoeck, R., Andrei, G., De Clercq, E. & Balzarini, J.
     Non-nucleoside structures retain full anti-HCMV potency of the dideoxy furanopyrimidine family.
     Antiviral Chem. Chemother., 15: 329-332 (2004).
     


603. Nawrot, B., Michalak, O., De Clercq, E. & Stec, W.J.
     Analogues of acyclic nucleosides derived from tris-(hydroxymethyl)phosphine oxide or bis-(hydroxymethyl)phosphinic acid coupled to DNA nucleobases.
     Antiviral Chem. Chemother., 15: 319-328 (2004).
     


604. Raić-Malić, S., Johayem, A., Ametamey, S.M., Batinac, S., De Clercq, E., Folkers, G. & Scapozza, L.
     Synthesis, 18F-radiolabelling and biological evaluations of C-6 alkylated pyrimidine nucleoside analogues.
     Nucleosides, Nucleotides and Nucleic Acids, 23: 1707-1721 (2004).
     


605. Voss, J., Wirsching, J., Schulze, O., Adiwidjaja, G., Giesler, A., Balzarini, J. & De Clercq, E.
     Thiosugars. XII. Synthesis of new 3’-O-substituted 2’,5’-anhydro-2’-thio-α-D-pentofuranosyl nucleoside analogues.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 1609-1623 (2004).
     


606. Chatgilialoglu, C., Ferreri, C., Gimisis, T., Gimisis, T., Roberti, M., Balzarini, J. & De Clercq, E.
     Synthesis and biological evaluation of novel 1’C-branched and spironucleoside analogues.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 1565-1581 (2004).
     


607. Caamano, O., Gómez, G., Fernández, F., García, M.D., García-Mera, X. & De Clercq, E.
     A convenient synthesis of new purinyl-homo-carbonucleosides on a cyclopentane ring fused with pyridazine.
     Synthesis, 2855-2862 (2004).
     


608. Balzarini, J., Pannecouque, C., Naesens, L., Andrei, G., Snoeck, R., De Clercq, E., Hocková, D.& Holý, A.
     6-[2-Phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines: a new class of acyclic pyrimidine nucleoside phosphonates with antiviral activity.
     Nucleosides, Nucleotides and Nucleic Acids, 23: 1321-1327 (2004).
     


609. De Clercq, E.
     Discovery and development of BVDU (brivudin) as a therapeutic for the treatment of herpes zoster.
     Biochem. Pharmacol., 68: 2301-2315 (2004).
     


610. Princen, K., Hatse, S., Vermeire, K., Aquaro, S., De Clercq, E., Gerlach, L.-O., Rosenkilde, M., Schwartz, T.W., Skerlj, R., Bridger, G. & Schols, D.
     Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist.
     J. Virol., 78: 12996-13006 (2004).
     


611. Zachariadis, P.C., Hadjikakou, S.K., Hadjiliadis, N., Skoulika, S., Michaelides, A., Balzarini, J. & De Clercq, E.
     Synthesis, characterization and in vitro study of the cytostatic and antiviral activity of new polymeric silver (I) complexes with ribbon structures derived from the conjugated heterocyclic thioamide 2-mercapto-3,4,5,6-tetrahydropyrimidine.
     Eur. J. Inorg. Chem., 1420-1426 (2004).
     


612. Fernández, F., García-Mera, X., Morales, M., Vilarino, L., Caamano, O. & De Clercq, E.
     Synthesis of new 6-substituted purinyl-5’-nor-1’-homocarbanucleosides based in indanol.
     Tetrahedron, 60: 9245-9253 (2004).
     


613. Figueira, M.J., Caamano, O., Fernández, F., Rodríguez-Borges, J.E., Balzarini, J. & De Clercq, E.
     Synthesis and biological evaluation of carbocyclic nucleosides with 2’,3’-dihomo-xylo-carbocyclic or carbocyclic fused to a tetrahydrofuran ring.
     Synthesis, 1991-1995 (2004).
     


614. Hatse, S., Princen, K., Vermeire, K., De Clercq, E. & Schols, D.
     Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studies..
     Cytometry, 61A: 178-188 (2004).
     


615. He, Y., Chen, F., Yu, X., Wang, Y., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Nonnucleoside HIV-1 reverse transcriptase inhibitors ; part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthyl-methyl)pyrimidin-4(3H)-ones.
     Bioorg. Chem., 32: 536-548 (2004).
     


616. Tabarrini, O., Stevens, M., Cecchetti, V., Sabatini, S., Dell’Uomo, M., Manfroni, G., Palumbo, M., Pannecouque, C., De Clercq, E. & Fravolini, A.
     Structure modifications of 6-aminoquinolones with potent anti-HIV activity.
     J. Med. Chem., 47: 5567-5578 (2004).
     


617. Maslen, H.L., Hughes, D., Hursthouse, M., De Clercq, E. Balzarini, J. & Simons, C.
     6-Azapyrimidine-2’-deoxy-4’-thionucleosides: antiviral agents against TK+ and TK- HSV and VZV strains.
     J. Med. Chem., 47: 5482-5491 (2004).
     


618. Vermeire, K., Princen, K., Hatse, S., De Clercq, E., Dey, K., Bell, T.W. & Schols, D.
     CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro.
     AIDS, 18: 2115-2125 (2004).
     


619. Wnuk, S.F., Lewandowska, E., Sacasa, P.R., Crain, L.N., Zhang, J., Borchardt, R.T. & De Clercq, E.
     Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects.
     J. Med. Chem., 47: 5251-5257 (2004).
     


620. Fikkert, V., Hombrouck, A., Van Remoortel, B., De Maeyer, M., Pannecouque, C., De Clercq, E., Debyser, Z. & Witvrouw, M.
     Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360
     AIDS, 18: 2019-2028 (2004).
     


621. De Clercq, E.
     Antiviral research at the Rega Institute (K.U.Leuven), now 50 years old.
     Antiviral Chem. Chemother., 15: 223-233 (2004).
     


622. De Bolle, L., Manichanh, C., Agut, H., De Clercq, E. & Naesens, L.
     Human herpesvirus 6 DNA polymerase: enzymatic parameters: sensitivity to ganciclovir and determination of the role of the A961V mutation in HHV-6 ganciclovir resistance.
     Antiviral Res., 64: 17-25 (2004).
     


623. Balzarini, J., Hatse, S., Vermeire, K., Princen, K., Aquaro, S., Perno, C.-F., De Clercq, E., Egberink, H., Vanden Mooter, G., Peumans, W., Vandamme, E. & Schols, D.
     Mannose-specific plant lectins from the Amaryllidaceae family qualify as efficient microbicides for prevention of human immunodeficiency virus infection.
     Antimicrob. Agents Chemother., 48: 3858-3870 (2004).
     


624. Selvam, P., Rajasekaran, A., Murugesh, N., Chandramohan, M. & De Clercq, E.
     Pharmacological screening of some novel isatin derivatives.
     Indian J. Pharm. Sci., 66: 465-469 (2004).
     


625. Balzarini, J., Van Laethem, K., Hatse, S., Vermeire, K., De Clercq, E., Peumans, W., Van Damme, E., Vandamme, A.-M., Böhlmstedt, A. & Schols, D.
     Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins.
     J. Virol., 78: 10617-10627 (2004).
     


626. De Clercq, E.
     Antivirals and antiviral strategies.
     Nature Rev. Microbiol., 2: 704-720 (2004).
     


627. Cutri, C.C.C., Garozzo, A., Pannecouque, C., Castro, A., Guerrera, F. & De Clercq, E.
     Isothiazole derivatives as novel HIV replication inhibitors.
     Antiviral Chem. Chemother., 15: 201-205 (2004).
     


628. Witvrouw, M., Van Maele, B., Vercammen, J., Hantson, A., Engelborghs, Y., De Clercq, E., Pannecouque, C. & Debyser, Z.
     Novel inhibitors of HIV-1 integration.
     Curr. Drug Metab., 5: 291-304 (2004).
     


629. Rao, A., Balzarini, J., Carbone, A., Chimirri, A., De Clercq, E., Monforte, A.M., Monforte, P., Pannecouque, C. & Zappalà, M.
     2-(2,6-Dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Antiviral Res., 63: 79-84 (2004).
     


630. Charlier, N., Leyssen, P., De Clercq, E. & Neyts, J.
     Rodent models for the study of therapy against flavivirus infections.
     Antiviral Res., 63: 67-77 (2004).
     


631. Delmas, F., Avellaneda, A., Di Giorgio, C., Robin, M., De Clercq, E., Timon-David, P. & Galy, J.-P.
     Synthesis and antileishmanial activity of (1,3-benzothiazol-2-yl)amino-9-(10H)-acridinone derivatives.
     Eur. J. Med. Chem., 39: 685-690 (2004).
     


632. Barreca, M.L., Rao, A., De Luca, L., Zappalà, M., Gurnari, C., Monforte, P., De Clercq, E., Van Maele, B., Debyser, Z., Witvrouw, M., Briggs, J.M. & Chimirri, A.
     Efficient 3D database screening for novel HIV-1 IN inhibitors.
     J. Chem. Inf. Comput. Sci., 44: 1450-1455 (2004).
     


633. De Clercq, E. & Neyts, J.
     Therapeutic potential of nucleoside/nucleotide analogues against poxvirus infections.
     Rev. Med. Virol., 14: 289-300 (2004).
     


634. Margiotta, N., Bergamo, A., Sava, G., Padovano, G., De Clercq, E. & Natile, G.
     Antiviral properties and cytotoxic activity of platinum(II) complexes with 1,10-phenanthrolines and acyclovir or penciclovir.
     J. Inorg. Biochem., 98: 1385-1390 (2004).
     


635. Kifli, N., De Clercq, E., Balzarini, J. & Simons, C.
     Novel imidazo[1,2-c]pyrimidine base-modified nucleosides: synthesis and antiviral activity evaluation.
     Bioorg. Med. Chem., 12: 4245-4252 (2004).
     


636. Liekens, S., Hernández, A.-I., Ribatti, D., De Clercq, E., Camarasa, M.-J., Pérez-Pérez, M.-J. & Balzarini, J.
     The nucleoside derivative 5’-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a non-competitive mechanism of action.
     J. Biol. Chem., 279: 29598-29605 (2004).
     


637. Auwerx, J., Stevens, M., Van Rompay, A.R., Bird, L.E., Ren, J., De Clercq, E., Öberg, B., Stammers, D.K., Karlsson, A. & Balzarini, J.
     The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT.
     J. Virol., 78: 7427-7437 (2004).
     


638. Charlier, N., Molenkamp, R., Leyssen, P., Paeshuyse, J., Drosten, C., Panning, M., De Clercq, E., Bredenbeek, P.J. & Neyts, J.
     Exchanging the yellow fever virus envelope proteins with Modoc virus prM and E proteins results in a chimeric virus that is neuroinvasive in SCID mice.
     J. Virol., 78: 7418-7426 (2004).
     


639. Taourirte, M., Ait Mohamed, L., Rochdi, A., Vasseur, J.J., Fernández, S., Ferrero, M., Gotor, V., Pannecouque, C., De Clercq, E. & Lazrek, H.B.
     Chemoenzymatic syntheses of homo- and heterodimers of AZT and d4T, and evaluation of their anti-HIV activity.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 701-714 (2004).
     


640. De Clercq, E.
     New anti-HIV agents in preclinical or clinical development.
     In: “Advances in Antiviral Drug Design”, volume 4, E. De Clercq (ed.), Elsevier Science B.V., London, United Kingdom, pp. 1-62 (2004).
     


641. De Clercq, E.
     Anti-HIV agents to be used in drug combination regimens.
     In: “Combination Therapy of AIDS”, E. De Clercq & A.-M. Vandamme (eds.). Birkhäuser Verlag, Switzerland, pp. 1-23 (2004).
     


642. Snoeck, R., De Clercq, E. & Andrei, G.
     Utilisation des antiviraux pour les orthopoxviroses.
     Médecine et Maladies Infectieuses, 34: S48-S50 (2004).
     


643. Velázquez, S., Lobatón, E., De Clercq, E., Koontz, D.L., Mellors, J.W., Balzarini, J. & Camarasa, M.-J.
     Hybrids of [TSAO-T]-[foscarnet]: the first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond.
     J. Med. Chem., 47: 3418-3426 (2004).
     


644. De Clercq, E.
     HIV-chemotherapy and –prophylaxis: new drugs, leads and approaches.
     Int. J. Biochem. Cell Biol., 36: 1800-1822 (2004).
     


645. Silvestri, M.A., Nagarajan, M., De Clercq, E., Pannecouque, C. & Cushman, M.
     Design, synthesis, anti-HIV activities, and metabolic stabilities of novel alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors.
     J. Med. Chem., 47: 3149-3162 (2004).
     


646. Baraldi, P.G., del Carmen Nunez, M., Tabrizi, M.A., De Clercq, E., Balzarini, J., Bermejo, J., Estévez, F. & Romagnoli, R.
     Design, synthesis, and biological evaluation of hybrid molecules containing -methylene--butyrolactones and polypyrrole minor groove binders.
     J. Med. Chem., 47: 2877-2886 (2004).
     


647. Kifli, N., Htar, T.T., De Clercq, E., Balzarini, J. & Simons, C.
     Novel bicyclic sugar modified nucleosides: synthesis, conformational analysis and antiviral evaluation.
     Bioorg. Med. Chem., 12: 3247-3257 (2004).
     


648. Hocková, D., Holý, A., Masojídková, M., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis and antiviral activity of 2,4-diamino-5-cyano-6-[2-(phosphonomethoxy)ethoxy] pyrimidine and related compounds.
     Bioorg. Med. Chem., 12: 3197-3202 (2004).
     


649. Neyts, J., Leyssen, P., Verbeken, E. & De Clercq, E.
     Efficacy of cidofovir in a murine model for disseminated/progressive vaccinia.
     Antimicrob. Agents Chemother., 48: 2267-2273 (2004).
     


650. Field, H.J. & De Clercq, E.
     Antiviral drugs – a short history of their discovery and development.
     Microbiology Today, 31: 58-61 (2004).
     


651. He, Y., Chen, F., Sun, G., Wang, Y., De Clercq, E., Balzarini, J. & Pannecouque, C.
     5-Alkyl-2-[(aryl and alkyloxycarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
     Bioorg. Med. Chem. Lett., 14: 3173-3176 (2004).
     


652. Angell, A., McGuigan, C., Garcia Sevillano, L., Snoeck, R., Andrei, G., De Clercq, E. & Balzarini, J.
     Bicyclic anti-VZV nucleosides: thieno analogues bearing an alkylphenyl side chain have reduced antiviral activity.
     Bioorg. Med. Chem. Lett., 14: 2397-2399 (2004).
     


653. Friedrichs, C., Neyts, J., Gaspar, G., De Clercq, E. & Wutzler, P.
     Evaluation of antiviral activity against human herpesvirus 8 (HHV-8) and Epstein-Barr virus (EBV) by a quantitative real-time PCR assay
     Antiviral Res., 62: 121-123 (2004).
     


654. De Clercq, E.
     Antiviral drugs in current clinical use
     J. Clin. Virol., 30: 115-133 (2004).
     


655. De Clercq, E.
     New anti-HIV agents in preclinical or clinical development.
     Frontiers in Medicinal Chemistry, 1: 543-579 (2004).
     


656. Holm, G.H., Zhang, C., Gorry, P.R., Peden, K., Schols, D., De Clercq, E. & Gabuzda, D.
     Apoptosis of bystander T cells induced by human immunodeficiency virus type 1 with increased envelope/receptor affinity and coreceptor binding site exposure.
     J. Virol., 78: 4541-4551 (2004).
     


657. Gerona-Navarro, G., Pérez de Vega, M.J., García-López, M.T., Andrei, G., Snoeck, R., Balzarini, J., De Clercq, E. & González-Muniz, R.
     Synthesis and anti-HCMV activity of 1-acyl--lactams and 1-acylazetidines derived from phenylalanine.
     Bioorg. Med. Chem. Lett., 14: 2253-2256 (2004).
     


658. Princen, K., Hatse, S., Vermeire, K., De Clercq, E. & Schols, D.
     Establishment of a novel CCR5 and CXCR4 expressing CD4+ cell line which is highly sensitive to HIV and suitable for high-throughput evaluation of CCR5 and CXCR4 antagonists.
     Retrovirology, 1: 2 (on line) (2004).
     


659. McGuigan, C., Pathirana, R.N., Snoeck, R., Andrei, G., De Clercq, E. & Balzarini, J.
     Discovery of a new family of inhibitors of human cytomegalovirus (HCMV) based upon lipophilic alkyl furano pyrimidine dideoxy nucleosides: action via a novel non-nucleosidic mechanism.
     J. Med. Chem., 47: 1847-1851 (2004).
     


660. Witvrouw, M., Pannecouque, C., Switzer, W., Folks, T.M., De Clercq, E. & Heneine, W.
     Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis.
     Antiviral Ther., 9: 57-65 (2004).
     


661. Van Griensven, J., Zhan, X., Van Maele, B., Pluymers, W., Michiels, M., De Clercq, E., Cherepanov, P. & Debyser, Z.
     Expression of HIV-1 integrase in CEM cells inhibits HIV-1 replication.
     J. Gene Med., 6: 268-277 (2004).
     


662. De Clercq, E.
     Nucleoside analogues exerting antiviral activity through a non-nucleoside mechanism.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 457-470 (2004).
     


663. Jakša, S., Kralj, B., Pannecouque, C., Balzarini, J., De Clercq, E. & Kobe, J.
     How a modification (8-aza-3-deaza-2’-deoxyguanosine) influences the quadruplex structure of Hotoda’s 6-mer TGG GAG with 5’- and 3’-end modifications.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 77-88 (2004).
     


664. Kumar, P., Ohkura, K., Balzarini, J., De Clercq, E., Seki, K.-i. & Wiebe, L.I.
     Synthesis and antiviral activity of novel fluorinated 2’,3’-dideoxynucleosides.
     Nucleosides, Nucleotides & Nucleic Acids, 23: 7-29 (2004).
     


665. McGuigan, C., Carangio, A., Snoeck, R., Andrei, G., De Clercq, E. & Balzarini, J.
     Synthesis and antiviral evaluation of some 3’-fluoro bicyclic nucleoside analogues.
     Nucleosides, Nucleotides, and Nucleic Acids, 23: 1-5 (2004).
     


666. Dimmock, J.R., Chamankhah, M., Das, U., Zello, G.A., Quail, J.W., Yang, J., Nienaber, K.H., Sharma, R.K., Selvakumar, P., Balzarini, J., De Clercq, E. & Stables, J.P.
     Cytotoxic and topographical properties of 6-arylidene-2-dimethylaminomethylcyclo-hexanone hydrochlorides and related compounds.
     J. Enzyme Inhibition Med. Chem., 19: 1-10 (2004).
     


667. Sienaert, R., Andrei, G., Snoeck, R., De Clercq, E., McGuigan, C. & Balzarini, J.
     Inactivity of the bicyclic pyrimidine nucleoside analogues against simian varicella virus (SVV) does not correlate with their substrate activity for SVV-encoded thymidine kinase.
     Biochem. Biophys. Res. Commun., 315: 877-883 (2004).
     


668. Gagnard, V., Leydet, A., Morère, A., Montero, J.L., Lefèbvre, I., Gosselin, G., Pannecouque, C. & De Clercq, E.
     Synthesis and in vitro evaluation of S-acyl-3-thiopropyl prodrugs of foscarnet.
     Bioorg. Med. Chem., 12: 1393-1402 (2004).
     


669. De Clercq, E.
     Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present and future.
     Chemistry & Biodiversity, 1: 44-64 (2004).
     


670. Anastasi, C., Hantz, O., De Clercq, E., Pannecouque, C., Clayette, P., Dereuddre-Bosquet, N., Dormont, D., Gondois-Rey, F., Hirsch, I. & Kraus, J.-L.
     Potent nonclassical nucleoside antiviral drugs based on the N,N-diarylformamidine concept.
     J. Med. Chem., 47: 1183-1192 (2004).
     


671. De Bolle, L., Hatse, S., Verbeken, E., De Clercq, E. & Naesens, L.
     Human herpesvirus 6 infection arrests cord blood mononuclear cells in G2 phase of the cell cycle.
     FEBS Lett., 560: 25-29 (2004).
     


672. Vashishtha, S.C., Zello, G.A., Nienaber, K.H., Balzarini, J., De Clercq, E., Stables, J.P. & Dimmock, J.R.
     Cytotoxic and anticonvulsant aryloxyaryl Mannich bases and related compounds.
     Eur. J. Med. Chem., 39: 27-35 (2004).
     


673. Selvam, P., Vanitha, K., Chandramohan, M. & De Clercq, E.
     Synthesis and antimicrobial activity of some novel 6-bromo-2-methyl/phenyl-3-(sulphonamido)quinazolin-4(3H)-ones.
     Indian J. Pharm. Sci., 66: 82-86 (2004).
     


674. Raić-Malić, S., Tomašković, L., Mrvoš-Sermek, D., Prugovecki, B., Cetina, M., Grdiša, M., Pavelić, K., Mannschreck, A., Balzarini, J., De Clercq, E. & Mintas, M.
     Spirobipyridopyrans, spirobinaphthopyrans, indolinospiropyridopyrans, indolinospironaphthopyrans and indolinospironaphtho-1,4-oxazines: synthesis, study of X-ray crystal structure, antitumoral and antiviral evaluation.
     Bioorg. Med. Chem., 12: 1037-1045 (2004).
     


675. Padalko, E., Verbeken, E., De Clercq, E. & Neyts, J.
     Inhibition of Coxsackie B3 virus induced myocarditis in mice by 2-(3,4-dichlorophenoxy)-5-nitrobenzonitrile.
     J. Med. Virol., 72: 263-267 (2004).
     


676. Andrei, G., De Clercq, E. & Snoeck, R.
     In vitro selection of drug-resistant varicella-zoster virus (VZV) mutants (OKA strain): differences between acyclovir and penciclovir ?
     Antiviral Res., 61: 181-187 (2004).
     


677. Rao, A., Balzarini, J., Carbone, A., Chimirri, A., De Clercq, E., Monforte, A.M., Monforte, P., Pannecouque, C. & Zappalà, M.
     Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
     Il Farmaco, 59: 33-39 (2004).
     


678. Auwerx, J., Esnouf, R., De Clercq, E. & Balzarini, J.
     Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors.
     Mol. Pharmacol., 65: 244-251 (2004).
     


679. Fonseca, T., Gigante, B., Marques, M.M., Gilchrist, T.L. & De Clercq, E.
     Synthesis and antiviral evaluation of benzimidazoles, quinoxalines and indoles from dehydroabietic acid.
     Bioorg. Med. Chem., 12: 103-112 (2004).
     


680. De Bolle, L., Andrei, G., Snoeck, R., Zhang, Y., Van Lommel, A., Otto, M., Bousseau, A., Roy, C., De Clercq, E. & Naesens, L.
     Potent, selective and cell-mediated inhibition of human herpesvirus 6 at an early stage of viral replication by the non-nucleoside compound CMV423
     Biochem. Pharmacol., 67: 325-336 (2004).
     


681. Padalko, E., Nuyens, D., De Palma, A., Verbeken, E., Aerts, J.L., De Clercq, E., Carmeliet, P. & Neyts, J.
     The interferon inducer ampligen [poly(I)-poly(C12U)] markedly protects mice against Coxsackie B3 virus-induced myocarditis.
     Antimicrob. Agents Chemother., 48: 267-274 (2004).
     



98 publications in the year 2003



682. Princen, K., Hatse, S., Vermeire, K., De Clercq, E. & Schols, D.
     Evaluation of SDF-1/CXCR4-induced Ca2+ signaling by fluorometric imaging plate reader (FLIPR) and flow cytometry.
     Cytometry, 51A: 35-45 (2003).
     


683. Esquieu, D., Péloponèse, J.-M., Opi, S., Gregoire, C., de Mareuil, J., Watkins, J., Campbell, G., Dunot, J.-P., Sturgis, J., Witvrouw, M., Pannecouque, C., De Clercq, E., Montembault, M., Giang, V.-T., Villiéras, M., Fargeas, V., Lebreton, J. & Loret, E.P.
     Discovery of a Tat HIV-1 inhibitor through computer-aided drug design.
     Spectroscopy, 17: 639-645 (2003).
     


684. Barreca, M.L., Chimirri, A., De Clercq, E., De Luca, L., Monforte, A.-M., Monforte, P., Rao, A. & Zappalà, M.
     Anti-HIV agents: design and discovery of new potent RT inhibitors.
     Il Farmaco, 58: 259-263 (2003).
     


685. Rao, A., Carbone, A., Chimirri, A., De Clercq, E., Monforte, A.M., Monforte, P., Pannecouque, C. & Zappalà.
     Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones.
     Il Farmaco, 58: 115-120 (2003).
     


686. Leyssen, P., Charlier, N., Paeshuyse, J., De Clercq, E. & Neyts, J.
     Prospects for antiviral therapy.
     In: “The Flaviviruses: Detection, Diagnosis and Vaccine Development”, T.J. Chamers & T.P. Monath (eds.). Advances in Virus Research, Elsevier B.V., Amsterdam, vol. 61, pp. 511-553 (2003).
     


687. Witvrouw, M., Pannecouque, C., Fikkert, V., Hantson, A., Van Remoortel, B., Hezareh, M., De Clercq, E. & Brown, S.J.
     Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entry.
     Antiviral Chem. Chemother., 14: 321-328 (2003).
     


688. Mager, P.P., De Clercq, E., Froeyen, M. & Reinhardt, R.
     Interactions of the dimeric triad of HIV-1 aspartyl protease with inhibitors.
     Drug Design & Discovery, 18: 53-64 (2003).
     


689. Princen, K., Hatse, S., Vermeire, K., Bridger, G.J., Skerlj, R.T., De Clercq, E. & Schols, D.
     The antiviral activity of the CXCR4 antagonist AMD3100 is independent of the cytokine-induced CXCR4/HIV coreceptor expression level.
     AIDS Res. Hum. Retrovir., 19: 1135-1139 (2003).
     


690. Zhao, Q., Lu, H., Schols, D., De Clercq, E. & Jiang, S.
     Development of a cell-based enzyme-linked immunosorbent assay for high-throughput screening of HIV-1 entry inhibitors targeting the coreceptor CXCR4.
     AIDS Res. Human Retroviruses, 19: 947-955 (2003).
     


691. Padalko, E., Verbeken, E., Matthys, P., Aerts, J., De Clercq, E. & Neyts, J
     Mycophenolate mofetil inhibits the development of Coxsackie B3-induced myocarditis in mice.
     BMC Microbiology, 3: 25 (pp. 1-9) (2003).
     


692. Prekupec, S., Svedružic, D., Gazivoda, T., Mrvoš-Sermek, D., Nagl, A., Grdiša, M., Pavelić, K., Balzarini, J., De Clercq, E., Folkers, G., Scapozza, L., Mintas, M. & Raić-Malić, S.
     Synthesis and biological evaluation of iodinated and fluorinated 9-(2-hydroxypropyl) and 9-(2-hydroxyethoxy)methyl purine nucleoside analogues.
     J. Med. Chem., 46: 5763-5772 (2003).
     


693. Stamatiou, G., Foscolos, G.B., Fytas, G., Kolocouris, A., Kolocouris, N., Pannecouque, C., Witvrouw, M., Padalko, E., Neyts, J. & De Clercq, E.
     Heterocyclic rimantadine analogues with antiviral activity.
     Bioorg. Med. Chem., 11: 5485-5492 (2003).
     


694. McGuigan, C., Brancale, A., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Novel bicyclic furanopyrimidines with dual anti-VZV and –HCMV activity.
     Bioorg. Med. Chem. Lett., 13: 4511-4513 (2003).
     


695. Barral, K., Hider, R.C., Balzarini, J., Neyts, J., De Clercq, E. & Camplo, M.
     Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxy-nucleoside derivatives.
     Bioorg. Med. Chem. Lett., 13: 4371-4374 (2003)
     


696. Maruyama, T., Kozai, S., Yamasaki, T., Witvrouw, M., Pannecouque, C., Balzarini, J., Snoeck, R., Andrei, G. & De Clercq, E.
     Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV.
     Antiviral Chem. Chemother., 14: 271-279 (2003)
     


697. Bonache, M.-C., Chamorro, C., Lobatón, E., De Clercq, E., Balzarini, J., Velázquez, S., Camarasa, M.-J. & San-Félix, A.
     Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors.
     Antiviral Chem. Chemother., 14: 249-262 (2003)
     


698. Hocková, D., Holý, A., Masojídková, M., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     5-Substituted-2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidines – acyclic nucleotide phosphonate analogues with antiviral activity.
     J. Med. Chem., 46: 5064-5073 (2003).
     


699. Russ, P., Schelling, P., Scapozza, L., Folkers, G., De Clercq, E. & Marquez, V.E.
     Synthesis and biological evaluation of 5-substituted derivatives of the potent antiherpes agent (North)-methanocarbathymine.
     J. Med. Chem., 46: 5045-5054 (2003).
     


700. De Clercq, E.
     Potentiel des phosphonates de nucléosides acycliques (cidofovir, adéfovir, ténofovir) dans le traitement des infections virales.
     Virologie, 7: S69-S86 (2003).
     


701. Fürstner, A., Albert, M., Mlynarski, J., Matheu, M. & De Clercq, E.
     Structure assignment, total synthesis, and antiviral evaluation of cycloviracin B1.
     J. Am. Chem. Soc., 125: 13132-13142 (2003).
     


702. Wirsching, J., Voss, J., Giesler, A., Kopf, J., Adiwidjaja, G., Balzarini, J. & De Clercq, E.
     Thiosugards. X. Novel nucleoside analogues derived from 4-thio-L-lyxofuranose.
     Nucleosides, Nucleotides and Nucleic Acids, 22: 1867-1897 (2003).
     


703. Lavandera, I., Fernández, S., Ferrero, M., De Clercq, E. & Gotor, V.
     Synthesis, protonation behavior, conformational analysis, and regioselective enzymatic acylation of the novel diamino analogue of (E)-5-(2-bromovinyl)-2’-deoxyuridine (BVDU).
     Nucleosides, Nucleotides and Nucleic Acids, 22: 1939-1952 (2003).
     


704. De Clercq, E.
     Clinical potential of acyclic nucleoside phosphonates cidofovir, adefovir, and tenofovir in treatment of DNA virus and retrovirus infections.
     Clin. Microbiol. Rev., 16: 569-596 (2003).
     


705. Fikkert, V., Van Maele, B., Vercammen, J., Hantson, A., Van Remoortel, B., Michiels, M., Gurnari, C., Pannecouque, C., Demaeyer, M., Engelborghs, Y., De Clercq, E., Debyser, Z. & Witvrouw, M.
     Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations.
     J. Virol., 77: 11459-11470 (2003).
     


706. 2025. Dinakaran, M., Selvam, P., De Clercq, E. & Sridhar, S.K.
     Synthesis, antiviral and cytotoxic activity of 6-bromo-2,3-disubstituted-4(3H)-quinazolinones.
     Biol. Pharm. Bull., 26: 1278-1282 (2003).
     


707. De Bolle, L., Balzarini, J., De Clercq, E. & Naesens, L.
     Characterization of the catalytic subunit of the human herpesvirus 6 (HHV-6) DNA polymerase expressed in an in vitro transcription/translation assay.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides and Nucleic Acids, 22: 999-1001 (2003).
     


708. Sienaert, R., Naesens, L., Brancale, A., Carangio, A., Andrei, G., Snoeck, R., Van Kuilenburg, A., De Clercq, E., McGuigan, C. & Balzarini, J.
     Metabolic and pharmacological characteristics of the bicyclic nucleoside analogues (BCNAs) as highly selective inhibitors of varicella-zoster virus (VZV).
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides and Nucleic Acids, 22: 995-997 (2003).
     


709. Moukha-chafiq, O., Taha, M.L., Mouma, A., Lazrek, H.B., Vasseur, J.J. & De Clercq, E.
     Synthesis and biological evaluation of some acyclic 4,6-disubstituted 1H-pyrazolo[3,4-d]pyrimidine nucleosides.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides and Nucleic Acids, 22: 967-972 (2003).
     


710. de Castro, S., Pérez-Pérez, M.-J., Lobatón, E., De Clercq, E., Balzarini, J., Camarasa, M.-J. & Velázquez, S.
     Unusual lability of 5’-O-tert-butyldimethylsilyl group on 4”-acyl TSAO derivatives.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 959-961 (2003).
     


711. Priego, E.M., Mendieta, J., Gago, F., Balzarini, J., De Clercq, E., Camarasa, M.-J. & Pérez-Pérez, M.-J.
     Towards new thymidine phosphorylase/PD-ECGF inhibitors based on the transition state of the enzyme reaction.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 951-953 (2003).
     


712. Bonache, M.-C., Chamorro, C., Velázquez, S., De Clercq, E., Balzarini, J., Camarasa, M.-J. & San-Félix, A.
     N-3 Substituted TSAO derivatives as a probe to explore the dimeric interface of HIV-1 reverse transcriptase.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 947-949 (2003).
     


713. Carangio, A., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus: synthesis and biological evaluation of 2’,3’-dideoxy-3’-fluoro and 2’-deoxy-xylo derivatives.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 935-937 (2003).
     


714. Luoni, G., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus: 5’-chloro and 3’-chloro derivatives.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 931-933 (2003).
     


715. Goslinski, T., Wenska, G., Golankiewicz, B., Balzarini, J. & De Clercq, E.
     Synthesis and fluorescent properties of 6-(4-biphenyl)-3,9-dihydro-9-oxo-5H-imidazo [1,2-A]purine analogues of acyclovir and ganciclovir.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 911-914 (2003).
     


716. Ermolinsky, B.S., Efimtseva, E.V., Alexeev, C.S., Mikhailov, S.N., Balzarini, J. & De Clercq, E.
     Dinucleoside monophosphates containing AZT and 1-methyladenosine or 7-methylgua-nosine.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 853-855 (2003).
     


717. Van Aerschot, A., Schepers, G., Busson, R., Neyts, J., De Clercq, E. & Herdewijn, P.
     Synthesis and antiviral evaluation of ribavirin congeners containing a hexitol moiety.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 849-851 (2003).
     


718. Gu, P., Morral, J., Wang, J., Rozenski, J., Busson, R., Van Aerschot, A., De Clercq, E. & Herdewijn, P.
     Synthesis and biological evaluation of a series of new cyclohexenyl nucleosides.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 845-847 (2003).
     


719. Lavandera, I., Fernández, S., Ferrero M, De Clercq, E. & Gotor, V.
     Synthesis and antiviral activity assay of novel (E)-3’,5’-diamino-5-(2-bromovinyl)-2’,3’,5’-trideoxyuridine.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 833-836 (2003).
     


720. Ait Mohamed, L., Taourirte, M., Rochdi, A., Lazrek, H.B., Vasseur, J.J., Engels, J.W., Pannecouque, C. & De Clercq, E.
     Synthesis of new homo and heterodimers of 2’,3’-dideoxyinosine (ddI) using ester linkages.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 829-831 (2003).
     


721. Meier, C., Renze, J.T., Balzarini, J. & De Clercq, E.
     d4TMP delivery from 7-substituted cycloSal-d4TMPs.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 825-827 (2003).
     


722. Bidet, O., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis of unusual bicyclic nucleosides bearing an unsaturated side-chain, as potential inhibitors of varicella-zoster virus (VZV).
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 817-819 (2003).
     


723. Muus, U., De Clercq, E., Balzarini, J., Naesens, L. & Meier, C.
     Study of different substituted cyclic and acyclic benzylpronucleotides of d4T relative to their hydrolytic stability and antiviral activity.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 791-795 (2003).
     


724. Terán, C., Santana, L., Uriarte, E., Vina, D. & De Clercq, E.
     Purine derivatives of 1,2-disubstituted cyclohexane analogues of nucleosides.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 787-789 (2003).
     


725. Barai, V.N., Zinchenko, A.I., Eroshevskaya, L.A., Zhernosek, E.V., Balzarini, J., De Clercq, E. & Mikhailopulo, I.A.
     Chemo-enzymatic synthesis of 3-deoxy--D-ribofuranosyl purines and study of their biological properties.
     Proceedings of the XV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, Leuven, Belgium, 10-14 September 2002.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 751-753 (2003).
     


726. Neyts, J. & De Clercq, E.
     Non-nucleoside inhibitors of HCMV replication.
     In: “New Aspects of CMV-Related Immunopathology”, Monographs in Virology, vol. 24, Prösch, S., Cinatl, J. & Scholz, M. (eds.), Karger AG, Basel, Switzerland, pp. 171-181 (2003).
     


727. Manfredini, S., Solaroli, N., Angusti, A., Nalin, F, Durini, E., Vertuani, S., Pricl, S., Ferrone, M., Spadari, S., Focher, F., Verri, A., De Clercq, E. & Balzarini, J.
     Design and synthesis of phosphonoacetic acid (PPA) ester and amide bioisosters of ribofuranosylnucleoside diphosphates as potential ribonucleotide reductase inhibitors and evaluation of their enzyme inhibitory, cytostatic and antiviral activity.
     Antiviral Chem. Chemother., 14: 183-194 (2003).
     


728. Galtier, C., Mavel, S., Snoeck, R., Andrei, G., Pannecouque, C., Witvrouw, M., Balzarini, J., De Clercq, E. & Gueiffier, A.
     Synthesis and antiviral activities of 3-aralkylthiomethylimidazo[1,2-b]pyridazine derivatives.
     Antiviral Chem. Chemother., 14: 177-182 (2003).
     


729. Hatse, S., Bridger, G., De Clercq, E. & Schols, D.
     X4 HIV-1 induces neuroblastoma cell death by interference with CXCL12/CXCR4 interaction.
     Cell. Mol. Biol., 49: OL443-OL452 (2003).
     


730. Cerasino, L., Intini, F.P., Kobe, J., De Clercq, E. &Natile, G.
     Synthesis and stereochemical characterisation of platinum(II) complexes with the antiviral agents penciclovir and famciclovir.
     Inorg. Chim. Acta, 344: 174-182 (2003).
     


731. Stevens, M., Pannecouque, C., De Clercq, E. & Balzarini, J.
     Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action.
     Antimicrob. Agents Chemother., 47: 3109-3116 (2003).
     


732. Dzolic, Z., Cetina, M., Kovacek, D., Hergold-Brundic, A., Mrvos-Sermek, D., Nagl, A., Slade, N., Pavelic, K., Balzarini, J., De Clercq, E., Zerbe, O., Folkers, G., Scapozza, L. & Mintas, M.
     Molecular structures and ab initio molecular orbital calculations of the optically active derivatives of 1-aminocyclopropane-1-carboxylic acid.
     J. Mol. Structure, 655: 229-241 (2003).
     


733. De Clercq, E.
     Nucleoside/nucleotide inhibitors of HIV reverse transcriptase.
     In: “Viral Infections and Treatment”, H. Rübsamen-Waigmann, K. Deres, G. Hewlett & R. Welker (eds.), Marcel Dekker, Inc., New York, pp. 485-504 (2003).
     


734. McGuigan, C., Jukes, A., Blewett, S., Barucki, H., Erichsen, J.T., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Halophenyl furanopyrimidines as potent and selective anti-VZV agents.
     Antiviral Chem. Chemother., 14: 165-170 (2003).
     


735. Zoidis, G., Kolocouris, N., Foscolos, G.B., Kolocouris, A., Fytas, G., Karayanis, P., Padalko, E., Neyts, J. & De Clercq, E.
     Are the 2-isomers of the drug rimantadine active anti-influenza A agents ?
     Antiviral Chem. Chemother., 14: 153-164 (2003).
     


736. Balzarini, J., De Clercq, E., Kaminska, B. & Orzeszko, A.
     Synthesis and antiviral activity of some 5’-N-phthaloyl-3’-azido-2’,3’-dideoxythymidine analogues.
     Antiviral Chem. Chemother., 14: 139-144 (2003).
     


737. Poznanski, J., Bretner, M., Kulikowski, T., Balzarini, J., Van Aerschot, A. & De Clercq, E.
     Synthesis, solution conformation and anti-HIV activity of novel 3’-substituted-2’,3’-dideoxy-5-hydroxymethyluridines and their 4,5-substituted analogues.
     Antiviral Chem. Chemother., 14: 127-138 (2003).
     


738. Blanco, J.M., Caamano, O., Fernández, F., Rodriguez-Borges, J.E., Balzarini, J. & De Clercq, E.
     Carbocyclic analogues of nucleosides from bis-(hydroxymethyl)cyclopentane: synthesis, antiviral and cytostatic activities of adenosine, inosine and uridine analogues.
     Chem. Pharm. Bull., 51: 1060-1063 (2003).
     


739. Maertens, G., Cherepanov, P., Pluymers, W., Busschots, K., De Clercq, E., Debyser, Z. & Engelborghs, Y.
     LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in humans cells.
     J. Biol. Chem., 278: 33528-33539 (2003).
     


740. Stevens, M., Pannecouque, C., De Clercq, E. & Balzarini, J.
     Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives.
     Antimicrob. Agents Chemother, 47: 2951-2957 (2003).
     


741. Leyssen, P., Croes, R., Rau, P., Heiland, S., Verbeken, E., Sciot, R., Paeshuyse, J., Charlier, N., De Clercq, E., Meyding-Lamadé, U. & Neyts, J.
     Acute encephalitis, a poliomyelitis-like syndrome and neurological sequelae in a hamster model for flavivirus infections.
     Brain Pathology, 13: 279-290 (2003).
     


742. Ying, C., De Clercq, E. & Neyts, J.
     Selective inhibition of hepatitis B virus replication by RNA interference.
     Biochem. Biophys. Res. Commun., 309: 482-484 (2003).
     2
     Ying, C., De Clercq, E. & Neyts, J.
     Selective inhibitors of hepatitis B virus replication.
     Curr. Med. Chem. - Anti-Infective Agents, 2: 227-240 (2003).
     


743. Coremans, G., Margaritis, V., Snoeck, R., Wyndaele, J., De Clercq, E. & Geboes, K.
     Topical cidofovir (HPMPC) is an effective adjuvant to surgical treatment of anogenital condylomata acuminata.
     Dis. Colon Rectum, 46: 1103-1109 (2003).
     


744. Dimmock, J.R., Jha, A., Zello, G.A., Sharma, R.K., Shrivastav, A., Allen, T.M., Santos, C.L., Balzarini, J., De Clercq, E., Manavathu, E.K. & Stables, J.P.
     3,5-Bis(phenylmethylene)-1-(N-arylmaleamoyl)-4-piperidones: a novel group of cytotoxic agents.
     J. Enzyme Inhibition Med. Chem., 18: 325-332 (2003).
     


745. Dimmock, J.R., Padmanilayam, M.P., Das, U., Zello, G.A., Sharma, R.K., Shrivastav, A., Selvakumar, P., Pasha, M.K., Nienaber, K.H., Lee, J.S., Allen, T.M., Santos, S.L., Balzarini, J. & De Clercq, E.
     Cytotoxic Mannich bases of 1-arylidene-2-tetralones.
     J. Enzyme Inhibition Med. Chem., 18: 313-324 (2003).
     


746. Dzolić, Z., Krištafor, V., Cetina, M., Nagl, A., Hergold-Brundić, A., Mrvoš-Sermek, D., Burgemeister, T., Grdiša, M., Slade, N., Pavelić, K., Balzarini, J., De Clercq, E. & Mintas, M.
     Synthesis, structural studies, and biological evaluation of some purine substituted 1-aminocyclopropane-1-carboxylic acids and 1-amino-1-hydroxymethylcyclopropanes.
     Nucleosides, Nucleotides & Nucleic Acids, 22: 373-389 (2003).
     


747. Simonart, T., Boelaert, J.R., Andrei, G., De Clercq, E. & Snoeck, R.
     Iron withdrawal strategies fail to prevent the growth of SiHa-induced tumors in mice.
     Gynecol. Oncol., 90: 91-95 (2003).
     


748. Anastasi, C., Vlieghe, P., Hantz, O., Schorr, O., Pannecouque, C., Witvrouw, M., De Clercq, E., Clayette, P., Dereuddre-Bosquet, N., Dormont, D., Gondois-Rey, F., Hirsch, I. & Kraus, J.-L.
     Are 5’-O-carbamate-2’,3’-dideoxythiacytidine new anti-HIV and anti-HBV nucleoside drugs or prodrugs ?
     Bioorg. Med. Chem. Lett., 13: 2459-2463 (2003).
     


749. Hatse, S., Princen, K., Vermeire, K., Gerlach, L.-O., Rosenkilde, M.M., Schwartz, T.W., Bridger, G., De Clercq, E. & Schols, D.
     Mutations at the CXCR4 interaction sites for AMD3100 influence anti-CXCR4 antibody binding and HIV-1 entry.
     FEBS Lett., 546: 300-306 (2003).
     


750. Balzarini, J., Pannecouque, C., De Clercq, E., Pavlov, A.Y., Printsevskaya, S.S., Miroshnikova, O.V., Reznikova, M.I. & Preobrazhenskaya, M.N.
     Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics.
     J. Med. Chem., 46: 2755-2764 (2003).
     


751. Meng, G., Chen, F.-E., De Clercq, E., Balzarini, J. & Pannecouque, C.
     Nonnucleoside HIV-1 reverse transcriptase inhibitors: part I. Synthesis and structure-activity relationship of 1-alkoxymethyl-5-alkyl-6-(1-naphthylmethyl)uracils as HEPT analogues.
     Chem. Pharm. Bull., 51: 779-789 (2003).
     


752. Neyts, J. & De Clercq, E.
     Therapy and short-term prophylaxis of poxvirus infections: historical background and perspectives.
     Antiviral Res., 57: 25-33 (2003).
     In:: “Handbook of Viral Bioterrorism & Biodefense”, E. De Clercq & E.R. Kern (eds.). Elsevier Science Publishers, Amsterdam, pp. 23-33 (2003).
     


753. De Clercq, E.
     The bicyclam AMD3100 story.
     Nature Rev. Drug Discovery, 2: 581-587 (2003).
     


754. Helliot, B., Panis, B., Frison, E., De Clercq, E., Swennen, R., Lepoivre, P. & Neyts, J.
     The acyclic nucleoside phosphonate analogues, adefovir, tenofovir and PMEDAP, efficiently eliminate banana streak virus from banana (Musa spp.).
     Antiviral Res., 59: 121-126 (2003).
     


755. Willey, S.J., Reeves, J.D., Hudson, R., Miyake, K., Dejucq, N., Schols, D., De Clercq, E., Bell, J., McKnight, A. & Clapham, P.R.
     Identification of a subset of human immunodeficiency virus type 1 (HIV-1), HIV-2, and simian immunodeficiency virus strains able to exploit an alternative coreceptor on untransformed human brain and lymphoid cells.
     J. Virol., 77: 6138-6152 (2003).
     


756. Dimmock, J.R., Jha, A., Zello, G.A., Allen, T.M., Santos, C.L., Balzarini, J., De Clercq, E., Manavathu, E.K. & Stables, J.P.
     Cytotoxic 4’-aminochalcones and related compounds.
     Pharmazie, 58: 227-232 (2003).
     


757. De Clercq, E.
     New inhibitors of HCMV (human cytomegalovirus) on the horizon
     J. Antimicrob. Chemother., 51: 1079-1083 (2003).
     


758. Suzutani, T., Ishioka, K., De Clercq, E., Ishibashi, K., Kaneko, H., Kira, T., Hashimoto, K.-i., Ogasawara, M., Ohtani, K., Wakamiya, N. & Wakamiya, N.
     Differential mutation patterns in thymidine kinase and DNA polymerase genes of herpes simplex virus type 1 clones passaged in the presence of acyclovir or penciclovir.
     Antimicrob. Agents Chemother., 47: 1707-1713 (2003).
     


759. Stylianakis, I., Kolocouris, A., Kolocouris, N., Fytas, G., Foscolos, G.B., Padalko, E., Neyts, J. & De Clercq, E.
     Spiro[pyrrolidine-2,2’-adamantanes]: synthesis, anti-influenza virus activity and conformational properties.
     Bioorg. Med. Chem. Lett., 13: 1699-1703 (2003).
     


760. Guillerm, G., Guillerm, D., Vandenplas-Vitkowski, C., Glapski, C. & De Clercq, E.
     Inactivation of S-adenosyl-L-homocysteine hydrolase with novel 5’-thioadenosine derivatives. Antiviral effects.
     Bioorg. Med. Chem. Lett., 13: 1649-1652 (2003).
     


761. Gu, P., Morral, J., Wang, J., Rozenski, J., Busson, R., Van Aerschot, A., De Clercq, E. & Herdewijn, P.
     Synthesis and antiviral activity of a series of new cyclohexenyl nucleosides.
     Antiviral Chem. Chemother., 14: 31-37 (2003).
     


762. Van Aerschot, A., Schepers, G., Busson, R., Rozenski, J., Neyts, J., De Clercq, E. & Herdewijn, P.
     Ribavirin derivatives with a hexitol moiety: synthesis and antiviral activity evaluation.
     Antiviral Chem. Chemother., 14: 23-30 (2003).
     


763. Jekle, A., Keppler, O.T., De Clercq, E., Schols, D., Weinstein, M. & Goldsmith, M.A.
     In vivo evolution of human immunodeficiency virus type 1 toward increased pathogenicity through CXCR4-mediated killing of uninfected CD4 T-cells.
     J. Virol., 77: 5846-5854 (2003).
     


764. De Clercq, E.
     Highly potent and selective inhibition of varicella-zoster virus replication by bicyclic furo [2,3-d]pyrimidine nucleoside analogues.
     Med. Res. Rev., 23: 253-274 (2003).
     


765. Leyssen, P., Paeshuyse, J., Charlier, N., Van Lommel, A., Drosten, C., De Clercq, E. & Neyts, J.
     Impact of direct virus-induced neuronal dysfunction and immunopathological damage on the progression of flavivirus (Modoc) encephalitis in a murine model.
     J. Neurovirol., 9: 69-78 (2003).
     


766. Lagoja, I.M., Pannecouque, C., Van Aerschot, A., Witvrouw, M., Debyser, Z., Balzarini, J., Herdewijn, P. & De Clercq, E.
     N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action.
     J. Med. Chem., 46: 1546-1553 (2003).
     


767. Van Maele, B., De Rijck, J., De Clercq, E. & Debyser, Z.
     Impact of the central polypurine tract on the kinetics of human immunodeficiency virus type 1 vector transduction.
     J. Virol., 77: 4685-4694 (2003).
     


768. Dimmock, J.R., Padmanilayam, M.P., Zello, G.A., Nienaber, K.H., Allen, T.M., Santos, C.L., De Clercq, E., Balzarini, J., Manavathu, E.K. & Stables, J.P.
     Cytotoxic analogues of 2,6-bis(arylidene)cyclohexanones.
     Eur. J. Med. Chem., 38: 169-177 (2003).
     


769. Okamoto, M., Wang, X., Debyser, Z., De Clercq, E. & Baba, M.
     Establishment of an in vitro assay system mimicking human immunodeficiency virus type 1-induced neural cell death and evaluation of inhibitors thereof.
     J. Virol. Methods, 108: 195-203 (2003).
     


770. Charlier, N., Molenkamp, R., Leyssen, P., Vandamme, A.-M., De Clercq, E., Bredenbeek, P. & Neyts, J.
     A rapid and convenient variant of fusion-PCR to construct chimeric flaviviruses.
     J. Virol. Methods, 108: 67-74 (2003).
     


771. Barreca, M.L., Chimirri, A., De Clercq, E., De Luca, L., Monforte, A.-M., Monforte, P., Rao, A. & Zappalà, M.
     Anti-HIV agents: design and discovery of new potent RT inhibitors.
     Il Farmaco, 58: 259-263 (2003).
     


772. Rao, A., Carbone, A., Chimirri, A., De Clercq, E., Monforte, A.M., Monforte, P., Pannecouque, C. & Zappalà.
     Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones.
     Il Farmaco, 58: 115-120 (2003).
     


773. Naimi, E., Zhou, A., Khalili, P., Wiebe, L.I., Balzarini, J., De Clercq, E. & Knaus, E.E.
     Synthesis of 3’- and 5’-nitrooxy pyrimidine nucleoside nitrate esters: “nitric oxide donor” agents for evaluation as anticancer and antiviral agents.
     J. Med. Chem., 46: 995-1004 (2003).
     


774. Leyssen, P., Drosten, C., Paning, M., Charlier, N., Paeshuyse, J., De Clercq, E. & Neyts, J.
     Interferons, interferon inducers, and interferon-ribavirin in treatment of flavivirus-induced encephalitis in mice.
     Antimicrob. Agents Chemother., 47: 777-782 (2003).
     


775. Cherepanov, P., Maertens, G., Proost, P., Devreese, B., Van Beeumen, J., Engelborghs, Y., De Clercq, E. & Debyser, Z.
     HIV-1 Integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells.
     J. Biol. Chem., 278: 372-381 (2003).
     


776. Vermeire, K., Bell, T.W., Choi, H.-J., Jin, Q., Samala, M.F., Sodoma, A., De Clercq, E. & Schols, D.
     The anti-HIV potency of cyclotriazadisulfonamide analogs is directly correlated with their ability to down-modulate the CD4 receptor.
     Mol. Pharmacol., 63: 203-210 (2003).
     


777. Princen, K., Hatse, S., Vermeire, K., De Clercq, E. & Schols, D.
     Evaluation of SDF-1/CXCR4-induced Ca2+ signaling by fluorometric imaging plate reader (FLIPR) and flow cytometry.
     Cytometry, 51A: 35-45 (2003).
     


778. De Clercq, E.
     Potential of acyclic nucleoside phosphonates in the treatment of DNA virus and retrovirus infections.
     Expert Rev. Anti-infect. Ther., 1: 21-43 (2003).
     


779. Armand-Ugón, M., Quinones-Mateu, M.E., Gutiérrez, A., Barretina, J., Blanco, J., Schols, D., De Clercq, E., Clotet, B. & Esté, J.A.
     Reduced fitness of HIV-1 resistant to CXCR4 antagonists.
     Antiviral Ther., 8: 1-8 (2003).
     



96 publications in the year 2002



780. De Clercq, E.
     New developments in anti-HIV chemotherapy.
     Proceedings of the “XXXVIIèmes Rencontres Internationales de Chimie Thérapeutique”, Tours, France, 4-6 July 2001.
     In: “Actualités de Chimie Thérapeutique”, Société de Chimie Thérapeutique, Châtenay-Malabry, France, pp. 61-82 (2002).
     


781. Snoeck, R. & De Clercq, E.
     New treatments for genital herpes.
     Curr. Opin. Infect. Dis., 15: 49-55 (2002).
     


782. Jung, M.E., Toyota, A., De Clercq, E. & Balzarini, J.
     Synthesis and biological activity of a series of methylene-expanded oxetanocin nucleoside analogues.
     Monatshefte für Chemie, 133: 499-520 (2002).
     


783. Iliopoulou, D., Roussis, V., Pannecouque, C., De Clercq, E. & Vagias, C.
     Halogenated sesquiterpenes from the red alga Laurencia obtusa.
     Tetrahedron, 58: 6749-6755 (2002).
     


784. Carangia, A., Srinivasan, S., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus: effect of terminal aryl substitution in the side-chain.
     Antiviral Chem. Chemother., 13: 263-271 (2002).
     


785. Dimmock, J.R., Jha, A., Zello, G.A., Quail, J.W., Oloo, E.O., Nienaber, K.H., Kowalczyk, E.S., Allen, T.M., Santos, C.L., De Clercq, E., Balzarini, J., Manavathu, E.K. & Stables, J.P.
     Cytotoxic N-[4-(3-aryl-3-oxo-1-propenyl)phenylcarbonyl]-3,5-bis(phenylmethylene)-4-piperidones and related compounds.
     Eur. J. Med. Chem., 37: 961-972 (2002).
     


786. Višnjevac, A., Tušek-Bozić, L., Majerić-Elenkov, M., Hameršak, Z., Koijman, H., De Clercq, E. & Kojić-Prodić, B.
     Synthesis, structural characterisation and biological activity of Zn(II) and Pd(II) complexes of 3-substituted 5-(2’-pyridyl)-1,4-benzodiazepin-2-one derivatives.
     Polyhedron, 21: 2567-2577 (2002).
     


787. Fikkert, V., Cherepanov, P., Van Laethem, K., Hantson, A., Van Remoortel, B., Pannecouque, C., De Clercq, E. Debyser, Z., Vandamme, A.-M. & Witvrouw, M.
     A new phenotypic assay to evaluate HIV susceptibility towards entry inhibitors
     Proceedings of the XIVth International AIDS Conference, Barcelona, Spain, 7-12 July 2002, pp. 19-22 (2002).
     


788. Van Vaerenbergh, K., De Geest, S., Derdelinckx, I., Bobbaers, H., Carbonez, A., Ceunen, H., De Graeve, V., De Saar, V., Deschamps, A., De Smet, K., Maes, B., Peetermans, W., Schrooten, Y., Desmyter, J., De Clercq, E., Van Ranst, M., Van Wijngaerden, E. & Vandamme, A.-M.
     A combination of poor adherence and a low baseline susceptibility score highly predictive for HAART failure.
     Antiviral Chem. Chemother., 13: 231-240 (2002).
     


789. Guenther, S., Balzarini, J., De Clercq, E. & Nair, V.
     A thymidine phosphorylase-stable analogue of BVDU with significant antiviral activity.
     J. Med. Chem., 45: 5426-5429 (2002).
     


790. Fikkert, V., Cherepanov, P., Van Laethem, K., Hantson, A., Van Remoortel, B., Pannecouque, C., De Clercq, E., Debyser, Z., Vandamme, A.-M. & Witvrouw, M.
     env Chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors
     Antimicrob. Agents Chemother., 46: 3954-3962 (2002).
     


791. Lakatosh, S.A., Balzarini, J., Andrei, G., Snoeck, R., De Clercq, E. & Preobrazhenskaya, M.N.
     Synthesis and cytotoxic activity of Nind-alkoxy derivatives of antibiotic arcyriarubin and dechloro-rebeccamycin aglycon.
     J. Antibiotics, 55: 768-773 (2002).
     


792. Rao, A., Chimirri, A., De Clercq, E., Monforte, A.M., Monforte, P., Pannecouque, C. & Zappalà, M.
     Synthesis and anti-HIV activity of 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzi-midazole structurally-related 1,2-substituted benzimidazoles.
     Il Farmaco, 57: 819-823 (2002).
     


793. Rao, A., Carbone, A., Chimirri, A., De Clercq, E., Monforte, A.M., Monforte, P., Pannecouque, C. & Zappalà, M.
     Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.
     Il Farmaco, 57: 747-751 (2002).
     


794. Barreca, M.L., Balzarini, J., Chimirri, A., De Clercq, E., De Luca, L., Höltje, H.D., Höltje, M., Monforte, A.M., Monforte, P., Pannecouque, C., Rao, A. & Zappalà, M.
     Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.
     J. Med. Chem., 45: 5410-5413 (2002).
     


795. Snoeck, R. & De Clercq, E.
     Role of cidofovir in the treatment of DNA virus infections, other than CMV infections, in immunocompromised patients.
     Curr. Opin. Invest. Drugs, 3: 1561-1566 (2002).
     


796. Dimmock, J.R., Padmanilyam, M.P., Zello, G.A., Quail, J.W., Oloo, E.O., Prisciak, J.S., Kraatz, H.-B., Cherkasov, A., Lee, J.S., Allen, T.M., Santos, C.L., Manuvathu, E.K., De Clercq, E., Balzarini, J. & Stables, J.P.
     Cytotoxic 1,3-diarylidene-2-tetralones and related compounds.
     Eur. J. Med. Chem., 37: 813-824 (2002).
     


797. Hillenkamp, J., Reinhard, T., Ross, R.S., Böhringer, D., Cartsburg, O., Roggendorf, M., De Clercq, E., Godehardt, E. & Sundmacher, R.
     The effects of cidofovir 1% with and without cyclosporin A 1% as a topical treatment of acute adenoviral keratoconjunctivitis. A controlled clinical pilot study.
     Ophthalmology, 109: 845-850 (2002).
     


798. Vermeire, K., Zhang, Y., Princen, K., Hatse, S., Samala, M., Dey, K., Choi, H.-J., Ahn, Y., Sodoma, A., Snoeck, R., Andrei, G., De Clercq, E., Bell, T.W. & Schols, D.
     CADA inhibits human immunodeficiency virus and human herpesvirus 7 replication by down-modulation of the cellular CD4 receptor.
     Virology, 302: 342-353 (2002).
     


799. Goslinski, T., Golankiewicz, B., De Clercq, E. & Balzarini, J.
     Synthesis and biological activity of the strongly fluorescent tricyclic analogues of acyclovir and ganciclovir.
     J. Med. Chem., 45: 5052-5057 (2002).
     


800. Mavel, S., Renou, J.-L., Galtier, C., Allouchi, H., Snoeck, R., Andrei, G., De Clercq, E., Balzarini, J. & Gueiffier, A.
     Influence of 2-substituent on the activity of imidazo[1,2-a]pyridine derivatives against human cytomegalovirus.
     Bioorg. Med. Chem., 10: 941-946 (2002).
     


801. Santana, L., Teijeira, M., Uriarte, E., Balzarini, J. & De Clercq, E.
     Synthesis, conformational analysis and antiviral and antitumoral activity of new 1,2-disubstituted carbocyclic nucleosides.
     Eur. J. Med. Chem., 37: 755-760 (2002).
     


802. Snoeck, R., Holý, A., Dewolf-Peeters, C., Van den Oord, J., De Clercq, E. & Andrei, G.
     Antivaccinia activity of acyclic nucleoside phosphonate derivatives in epithelial cells and organotypic cultures.
     Antimicrob. Agents Chemother., 46: 3356-3361 (2002).
     


803. Garuti, L., Roberti, M. & De Clercq, E.
     Synthesis and antiviral/antiproliferative activity of some N-sulphonylbenzimidazoles.
     Bioorg. Med. Chem. Lett., 12: 2707-2710 (2002).
     


804. Daelemans, D., Afonina, E., Nilsson, J., Werner, G. Kjems, J., De Clercq, E., Pavlakis, G.N. & Vandamme, A.-M.
     A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export
     Proc. Natl. Acad. Sci. USA, 99: 14440-14445 (2002).
     


805. Saijo, M., Suzutani, T., De Clercq, E., Niikura, M., Maeda, A., Morikawa, S. & Kurane, I.
     Genotypic and phenotypic characterization of the thymidine kinase of ACV-resistant HSV-1 derived from an acyclovir-sensitive herpes simplex virus type 1 strain.
     Antiviral Res., 56: 253-262 (2002).
     


806. Moukha-chafiq, O., Taha, M.L., Lazrek, H.B., Vasseur, J.J., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and biological activity of some 4-substituted 1-[1-(2,3-dihydroxy-1-propoxy)methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
     Il Farmaco, 57: 27-32 (2002).
     


807. Vercammen, J., Maertens, G., Gerard, M., De Clercq, E., Debyser, Z. & Engelborghs.
     DNA-induced polymerization of HIV-1 integrase analyzed with fluorescence fluctuation spectroscopy.
     J. Biol. Chem., 277: 38045-38052 (2002).
     


808. Gáspár, G., De Clercq, E. & Neyts, J.
     Gammaherpesviruses encode functional dihydrofolate reductase activity.
     Biochem. Biophys. Res. Commun., 297, 756-759 (2002).
     


809. Hilgeroth, A., Molnár, J. & De Clercq, E.
     Using molecular symmetry to form new drugs: hydroxymethyl-substituted 3,9-diazatetraasteranes as the first class of symmetric MDR modulators.
     Angew. Chem. Int. Ed., 41: 3623-3625 (2002).
     


810. Bergstrom, D.E., Lin, X., Wood, T.D., Witvrouw, M., Ikeda, S., Andrei, G., Snoeck, R., Schols, D. & De Clercq, E.
     Polysulfonates derived from metal thiolate complexes as inhibitors of HIV-1 and various other enveloped viruses in vitro.
     Antiviral Chem. Chemother., 13: 185-195 (2002).
     


811. Ying, C., Van Pelt, J.F., Van Lommel, A., Van Ranst, M., Leyssen, P., De Clercq, E. & Neyts, J.
     Sulphated and sulphonated polymers inhibit the initial interaction of hepatitis B virus with hepatocytes.
     Antiviral Chem. Chemother., 13: 157-164 (2002).
     


812. Charlier, N., Leyssen, P., Paeshuyse, J., Drosten, C., Schmitz, H., Van Lommel, A., De Clercq, E. & Neyts, J.
     Infection of SCID mice with Montana myotis leukoencephalitis virus as a model for flavivirus encephalitis.
     J. Gen. Virol., 83: 1887-1896 (2002).
     


813. Charlier, N., Leyssen, P., Pleij, C.W.A., Lemey, P., Billoir, F., Van Laethem, K., Vandamme, A.-M., De Clercq, E., de Lamballerie, X. & Neyts, J.
     Complete genome sequence of Montana myotis leukoencephalitis virus, phylogenetic analysis and comparative study of the 3’ untranslated region of flaviviruses with no known vector.
     J. Gen. Virol., 83: 1875-1885 (2002).
     


814. Salido, S., Altarejos, J., Nogueras, M., Sánchez, A., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Chemical studies of essential oils of Juniperus oxycedrus ssp. badia.
     J. Ethnopharmacol., 81: 129-134 (2002).
     


815. Pluymers, W., Pais, G., Van Maele, B., Pannecouque, C., Fikkert, V., Burke, T.R. Jr., De Clercq, E., Witvrouw, M., Neamati, N. & Debyser, Z.
     Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives.
     Antimicrob. Agents Chemother., 46: 3292-3297 (2002).
     


816. De Clercq, E.
     Cidofovir in the therapy and short-term prophylaxis of poxvirus infections.
     Trends Pharmacol. Sci., 23: 456-458 (2002).
     


817. Gáspár, G., De Clercq, E. & Neyts, J.
     Human herpesvirus 8 gene encodes a functional thymidylate synthase.
     J. Virol., 76: 10530-10532 (2002).
     


818. Manallack, D.T., Pitt, W.R., Herdewijn, P., Balzarini, J., De Clercq, E., Sanderson, M.R., Sohi, M., Wien, F., Munier-Lehmann, H., Haouz, A. & Delarue, M.
     Database searching for thymidine and thymidylate kinase inhibitors using three-dimensional structure-based methods.
     J. Enzyme Inhibition Med. Chem., 17: 167-174 (2002).
     


819. De Clercq, E.
     New anti-HIV agents and targets.
     Med. Res. Rev., 22: 531-565 (2002).
     


820. Hatse, S., Princen, K., Bridger, G., De Clercq, E. & Schols, D.
     Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4.
     FEBS Lett., 527: 255-262 (2002).
     


821. De Clercq, E.
     New developments in anti-HIV chemotherapy.
     Proceedings of the 8th International Symposium on Molecular Aspects of Chemotherapy, Gdansk, Poland, 5-9 September 2001.
     Biochim. Biophys. Acta, 1587: 258-275 (2002).
     


822. De Clercq, E.
     Antiviral activity of nucleoside analogues: the BVDU connection”.
     In: “Recent Advances in Nucleosides: Chemistry and Chemotherapy”, D. Chu (ed.). Elsevier Science B.V., New York, NY, USA, pp 433-454 (2002).
     


823. De Bolle, L., Michel, D., Mertens, T., Manichanh, C., Agut, H., De Clercq, E. & Naesens, L.
     Role of the human herpesvirus 6 U69-encoded kinase in the phosphorylation of ganciclovir.
     Mol. Pharmacol., 62: 714-721 (2002).
     


824. Balzarini, J., Ostrowski, T., Goslinski, T., De Clercq, E. & Golankiewicz.
     Pronounced cytostatic activity and bystander effect of a novel series of fluorescent tricyclic acyclovir and ganciclovir derivatives in herpes simplex virus thymidine kinase gene-transduced tumor cell lines.
     Gene Ther., 9: 1173-1182 (2002).
     


825. Snoeck, R., Andrei, G., Bodaghi, B., Lagneaux, L., Daelemans, D., De Clercq, E., Neyts, J., Schols, D., Naesens, L., Michelson, S., Bron, D., Otto, M.J., Bousseau, A., Nemecek, C. & Roy, C.
     2-Chloro-3-pyridin-3-yl-5,6,7,8-tetrahydroindolizine-1-carboxamide (CMV423), a new lead compound for the treatment of human cytomegalovirus infections.
     Antiviral Res., 55: 413-424 (2002).
     


826. Lobatón, E., Rodríguez-Barrios, F., Gago, F., Pérez-Pérez, M.-J., De Clercq, E., Balzarini, J., Camarasa, M.-J. & Velázquez, S.
     Synthesis of 3”-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.
     J. Med. Chem., 45: 3934-3945 (2002).
     


827. Ducho, C., Balzarini, J., Naesens, L., De Clercq, E. & Meier, C.
     Aryl-substituted and benzo-annulated cycloSal-derivatives of 2’,3’-dideoxy-2’,3’-didehydrothymidine monophosphate – correlation of structure, hydrolysis properties and anti-HIV activity.
     Antiviral Chem. Chemother., 13: 129-141 (2002).
     


828. Meier, C., Muus, U., Renze, J., Naesens, L., De Clercq, E. & Balzarini, J.
     Comparative study of bis(benzyl)phosphate triesters of 2’,3’-dideoxy-2’,3’-didehydrothymidine (d4T) and cycloSal-d4TMP – hydrolysis, mechanistic insights and anti-HIV activity.
     Antiviral Chem. Chemother., 13: 101-114 (2002).
     


829. McGuigan, C., Blewett, S., Siccardi, D., Erichsen, J.T., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Alkyloxyphenyl furano pyrimidines as potent and selective anti-VZV agents with enhanced water solubility.
     Antiviral Chem. Chemother., 13: 91-99 (2002).
     


830. Van Gelder, J., Deferme, S., Naesens, L., De Clercq, E., Van den Mooter, G., Kinget, R. & Augustijns, P.
     Intestinal absorption enhancement of the ester prodrug tenofovir disoproxil fumarate through modulation of the biochemical barrier by defined ester mixtures.
     Drug Metabolism & Disposition, 30: 924-930 (2002).
     


831. Neyts, J., Verbeken, E. & De Clercq, E.
     Effect of 5-iodo-2’-deoxyuridine on vaccinia virus (orthopoxvirus) infections in mice.
     Antimicrob. Agents Chemother., 46: 2842-2847 (2002).
     


832. Pannecouque, C., Pluymers, W., Van Maele, B., Tetz, V., Cherepanov, P., De Clercq, E., Witvrouw, M. & Debyser, Z.
     New class of inhibitors of HIV integrase inhibitors that block viral replication in cell culture.
     Curr. Biol., 12: 1169-1177 (2002).
     


833. Balzarini, J., Stevens, M., Andrei, G., Snoeck, R., Strunk, R., Pierce, J.B., Lacadie, J.A., De Clercq, E. & Pannecouque, C.
     Pyridine oxide derivatives: structure-activity relationship for inhibition of human immunodeficiency virus and cytomegalovirus replication in cell culture.
     Helv. Chim. Acta, 85: 2961-2974 (2002).
     


834. Barai, V.N., Zinchenko, A.I., Eroshevskaya, L.A., Zhernosek, E.V., De Clercq, E. & Mikhailopulo, I.A.
     Chemo-enzymatic synthesis of 3-deoxy--D-ribofuranosyl purines.
     Helv. Chim. Acta, 85: 1893-1900 (2002).
     


835. Lagoja, I.M., Pannecouque, C., Musumeci, L., Froeyen, M., Van Aerschot, A., Balzarini, J., Herdewijn, P. & De Clercq, E.
     1,2,4-Triazole derivatives inhibiting the human immunodeficiency virus type 1 (HIV-1) in vitro.
     Helv. Chim. Acta, 85: 1883-1892 (2002).
     


836. Witvrouw, M. & De Clercq, E.
     HIV entry as antiviral strategy.
     In: “Viral Entry and the Pathogenesis of AIDS”, J.A. Esté & B. Clotet (eds.), Hospital Universitari Germans Trias I Pujol, Badalona, Spain, pp. 137-160 (2002).
     


837. Saijo, M., Yasuda, Y., Yabe, H., Kato, S., Suzutani, T., De Clercq, E., Niikura, M., Maeda, A., Kurane, I. & Morikawa, S.
     Bone marrow transplantation in a child with Wiskott-Aldrich syndrome latently infected with acyclovir-resistant (ACVr) herpes simplex virus type 1: emergence of foscarnet-resistant virus originating from the ACVr virus.
     J. Med. Virol., 68: 99-104 (2002).
     


838. Balzarini, J., Sienaert, R., Liekens, S., Van Kuilenburg, A., Carangio, A., Esnouf, R., De Clercq, E. & McGuigan, C.
     Lack of susceptibility of bicyclic nucleoside analogs, highly potent inhibitors of varicella-zoster virus, to the catabolic action of thymidine phosphorylase and dihydropyrimidine dehydrogenase.
     Mol. Pharmacol., 61: 1140-1145 (2002).
     


839. Balzarini, J., Pannecouque, C., De Clercq, E., Aquaro, S., Perno, C.-F., Egberink, H. & Holý, A.
     Antiretrovirus activity of a novel class of acyclic pyrimidine nucleoside phosphonates.
     Antimicrob. Agents Chemother., 46: 2185-2193 (2002).
     


840. Dimmock, J.R., Zello, G.A., Oloo, E.O., Quail, J.W., Kraatz, H.-B., Perjési, P., Aradi, F., Takács-Novák, K., Allen, T.M., Santos, C.L., Balzarini, J., De Clercq, E. & Stables, J.P.
     Correlations between cytotoxicity and topography of some 2-arylidenebenzocyclo-alkanones determined X-ray crystallography.
     J. Med. Chem., 45: 3103-3111 (2002).
     


841. Debyser, Z., Cherepanov, P., Van Maele, B., De Clercq, E. & Witvrouw, M.
     In search of authentic inhibitors of HIV-1 integration.
     Antiviral Chem. Chemother., 13: 1-15 (2002).
     


842. Simonart, T., Boelaert, J.R., Andrei, G., van den Oord, J.J., Degraef, C., Hermans, P., Noel, J.-C., Van Vooren, J.-P., Heenen, M., De Clercq, E. & Snoeck, R.
     Desferrioxamine enhances AIDS-associtated Kaposi’s sarcoma tumor development in a xenograft model.
     Int. J. Cancer., 100: 140-143 (2002).
     


843. Wirsching, J., Schulze, O., Voss, J., Giesler, A., Kopf, J., Adiwidjaja, G., Balzarini, J. & De Clercq, E.
     Synthesis and biological evaluation of isonucleosides derived from methyl 3,5-anhydro-2-O-(2-fluorobenzyl)-D-xylofuranosides.
     Nucleosides, Nucleotides & Nucleic Acids, 21: 257-274 (2002).
     


844. Nieto, M.I., Caamano, O., Fernández, F., Gómez, M., Balzarini, J. & De Clercq, E.
     Synthesis, antiviral and cytostatic activities, of carbocyclic nucleosides incorporating a modified cyclopentane ring. IV. Adenosine and uridine analogues.
     Nucleosides, Nucleotides & Nucleic Acids, 21: 243-255 (2002).
     


845. Vogel, J.-U., Michaelis, M., Neyts, J., Blaheta, R.A., Snoeck, R., Andrei, G., De Clercq, E., Rabenau, H.F., Kreuter, J., Cinatl Jr., J. & Doerr, H.W.
     Antiviral and immunomodulatory activity of the metal chelator ethylenediaminedisuccinic acid against cytomegalovirus in vitro and in vivo.
     Antiviral Res., 55: 179-188 (2002).
     


846. De Clercq, E.
     Cidofovir in the treatment of poxvirus infections.
     Antiviral Res., 55: 1-13 (2002).
     


847. Jekle, A., Schramm, B., Jayakumar, P., Trautner, V., Schols, D., De Clercq, E., Mills, J., Crowe, S.M. & Goldsmith, M.A.
     Coreceptor phenotype of natural human immunodeficiency virus with Nef deleted evolves in vivo, leading to increased virulence.
     J. Virol., 76: 6966-6973 (2002).
     


848. Fernández, F., García-Mera, X., Morales, M., Rodríguez-Borges, J.E. & De Clercq, E.
     Synthesis and cytostatic activities of new 6-substituted purinylcarbonucleosides derived from indan.
     Synthesis, 2002: 1084-1090 (2002).
     


849. Wnuk, S.F., Ro, B.-O., Valdez, C.A., Lewandowska, E., Valdez, N.X., Sacasa, P.R., Yin, D., Zhang, J., Borchardt, R.T. & De Clercq, E.
     Sugar-modified conjugated diene analogues of adenosine and uridine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects.
     J. Med. Chem., 45: 2651-2658 (2002).
     


850. Balzarini, J., Liekens, S., Esnouf, R. & De Clercq, E.
     The A167Y mutation converts the herpes simplex virus type 1 thymidine kinase into a guanosine analogue kinase.
     Biochemistry, 41: 6517-6524 (2002).
     


851. Kritsanida, M., Mouroutsou, A., Marakos, P., Pouli, N., Papakonstantinou-Garoufalias, S., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
     Il Farmaco, 57: 253-257 (2002).
     


852. Stragier, I., Snoeck, R., De Clercq, E., Van den Oord, J.J., Van Ranst, M. & Degreef, H.
     Local treatment of HPV-induced skin lesions by cidofovir.
     J. Med. Virol., 67: 241-245 (2002).
     


853. De Clercq, E.
     Highlights in the development of new antiviral agents.
     Mini-Rev. Med. Chem., 2: 163-175 (2002).
     


854. Martinez, A., Gil, C., Castro, A., Perez, C., Witvrouw, M., Pannecouque, C., Balzarini, J. & De Clercq, E.
     Anti-HIV-1 activity of benzothiadiazine dioxide.
     Antiviral Chem. Chemother., 12: 347-351 (2002).
     


855. Meerbach, A., Neyts, J., Balzarini, J., Helbig, B., De Clercq, E. & Wutzler, P.
     In vitro activity of polyhydroxycarboxylates against herpesviruses and HIV.
     Antiviral Chem. Chemother., 12: 337-345 (2002).
     


856. Van Gelder, J., Van den Mooter, G., De Clercq, E. & Augustijns, P.
     Metabolism of ester prodrugs by enzymes present in the intestinal lumen.
     Proceedings of the 4th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, Florence, Italy, 8-11 April 2000, pp. 729-730 (2002).
     


857. Tronchet, J.M.J., Chalard, F., Rivara-Minten, E., Seman, M., De Clercq, E., Balzarini, J. & Dilda, P.
     Synthesis and in vitro cytotoxic and antiviral activities of 1-(2,5,6-trideoxy-6-halogenohept-5-enofuranurononitrile)thymine and derivatives.
     Nucleosides, Nucleotides & Nucleic Acids, 21: 191-206 (2002).
     


858. Holý, A., Votruba, I., Masojídková, Andrei, G., Snoeck, R., Naesens, L., De Clercq, E. & Balzarini, J.
     6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with antiviral activity.
     J. Med. Chem., 45: 1918-1929 (2002).
     


859. De Clercq, E.
     A voyage of discovery in viral chemotherapy.
     Newsletter of the International Society of Chemotherapy, 6: 4-5 (2002).
     


860. Van Vaerenbergh, K., Harrer, T., Schmit, J.-C., Carbonez, A., Fontaine, E., Kurowski, M., Grünke, M., Löw, P., Rascu, A., Schmidt, B., Schmitt, M., Thoelen, I., Walter, H., Van Laethem, K., Van Ranst, M., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
     Initiation of HAART in drug-naive HIV type 1 patients prevents viral breakthrough for a median period of 35.5 months in 60% of the patients.
     AIDS Res. Hum. Retrovir., 18: 419-426 (2002).
     


861. Moukha-chafiq, O., Taha, M.L., Lazrek, H.B., Vasseur, J.J. & De Clercq, E.
     Synthesis and biological evaluation of some acyclic -(1H-pyrazolo[3,4-d]pyrimidin-4-ylthio)alkylamide nucleosides.
     Nucleosides, Nucleotides & Nucleic Acids, 21: 165-176 (2002).
     


862. Simonart, T., Boelaert, J.R., Mosselmans, R., Andrei, G., Noel, J.C., De Clercq, E. & Snoeck, R.
     Antiproliferative and apoptotic effects of iron chelators on human cervical carcinoma cells.
     Gynecol. Oncol., 85: 95-102 (2002).
     


863. Snoeck, J., Van Dooren, S., Van Laethem, K., Derdelinckx, I., Van Wijngaerden, E., De Clercq, E. & Vandamme, A.-M.
     Prevalence and origin of HIV-1 group M subtypes among patients attending a Belgian hospital in 1999.
     Virus. Res., 85: 95-107 (2002).
     


864. Vlieghe, P., Clerc, T., Pannecouque, C., Witvrouw, M., De Clercq, E., Salles, J.-P. & Kraus, J.-L.
     Synthesis of new covalently bound -carrageenan-AZT conjugates with improved anti-HIV activities.
     J. Med. Chem., 45: 1275-1283 (2002).
     


865. Dimmock, J.R., Jha, A., Kumar, P., Zello, G.A., Quail, J.W., Oloo, E.O., Oucharek, J.J., Pasha, M.K., Seitz, D., Sharma, R.K., Allen, T.M., Santos, C.L., Manavathu, E.K., De Clercq, E., Balzarini, J. & Stables, J.P.
     Cytotoxic 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes and related compounds.
     Eur. J. Med. Chem., 37: 35-44 (2002).
     


866. Deferme, S., Van Gelder, J., Ingels, F., Van den Mooter, G., De Buck, S., Balzarini, J., Naesens, L., De Clercq, E., Kinget, R. & Augustijns, P.
     Intestinal absorption characteristics of the low solubility thiocarboxanilide UC-781.
     Int. J. Pharm., 234: 113-119 (2002).
     


867. Naif, H.M., Cunningham, A.L., Alali, M., Li, S., Nasr, N., Buhler, M.M., Schols, D., De Clercq, E. & Stewart, G.
     A human immunodeficiency virus type 1 isolate from an infected person homozygous for CCR532 exhibits dual tropism by infecting macrophages and MT2 cells via CXCR4.
     J. Virol., 76: 3114-3124 (2002).
     


868. Cos, P., Hermans, N., De Bruyne, T., Apers, S., Sindambiwe, J.B., Witvrouw, M., De Clercq, E., Vanden Berghe, D., Pieters, L. & Vlietinck, A.J.
     Antiviral activity of Rwandan medicinal plants against human immunodeficiency virus type-1 (HIV-1).
     Phytomedicine, 9: 62-68 (2002).
     


869. Kolocouris, A., Dimas, K., Pannecouque, C., Witvrouw, M., Foscolos, G.B., Stamatiou, G., Fytas, G., Zoidis, G., Kolocouris, N., Andrei, G., Snoeck, R. & De Clercq, E.
     New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones – thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
     Bioorg. Med. Chem. Lett., 12: 723-727 (2002).
     


870. Leyssen, P., Charlier, N., Lemey, P., Billoir, F., Vandamme, A.-M., De Clercq, E., de Lamballerie, X. & Neyts, J.
     Complete genome sequence, taxonomic assignment and comparative analysis of the untranslated regions of the Modoc virus, a flavivirus with no known vector.
     Virology, 293: 125-140 (2002).
     


871. Auwerx, J., North, T.W., Preston, B.D., Klarmann, G.J., De Clercq, E. & Balzarini, J.
     Chimeric human immunodeficiency virus type 1 and feline immunodeficiency virus reverse transcriptases: role of the subunits in resistance/sensitivity to non-nucleoside reverse transcriptase inhibitors.
     Mol. Pharmacol., 61: 400-406 (2002).
     


872. Sienaert, R., Naesens, L., Brancale, A., De Clercq, E., McGuigan, C. & Balzarini, J.
     Specific recognition of the bicyclic pyrimidine nucleoside analogs, a new class of highly potent and selective inhibitors of varicella-zoster virus (VZV), by the VZV-encoded thymidine kinase.
     Mol. Pharmacol., 61: 249-254 (2002).
     


873. Liekens, S., Bilsen, F., De Clercq, E., Priego, E.M., Camarasa, M.-J., Pérez-Pérez, M.-J. & Balzarini, J.
     Anti-angiogenic activity of a novel multisubstrate analogue inhibitor of thymidine phosphorylase.
     FEBS Lett., 510: 83-88 (2002).
     


874. Das, S.R., Schneller, S.W., Balzarini, J. & De Clercq, E.
     A mercapto analogue of 5’-noraristeromycin.
     Bioorg. Med. Chem., 10: 457-460 (2002).
     


875. De Clercq, E.
     Strategies in the design of antiviral drugs.
     Nature Reviews Drug Discovery, 1: 13-25 (2002).
     



123 publications in the year 2001



876. Garoufis, A., Karidi, K., Hadjiliadis, N., Kasselouri, S., Kobe, J., Balzarini, J. & De Clercq, E.
     Synthesis, characterization and antiviral properties of Pd(II) complexes with penciclovir.
     Metal Based Drugs, 8: 57-63 (2001).
     


877. Nakagaki, K., Nakagaki, K., Takahashi, K., Schols, D., De Clercq, E. & Tabira, T.
     CXCR4 is the primary receptor for feline immunodeficiency virus in astrocytes.
     J. Neurovirol., 7: 487-492 (2001).
     


878. Chaouni-Benabdallah, A., Galtier, C., Allouchi, H., Kherbeche, A., Chavignon, O., Teulade, J.-C., Witvrouw, M., Pannecouque, C., Snoeck, R., Andrei, G., Balzarini, J., De Clercq, E., Fauvelle, F., Enguehard, C. & Gueffier, A.
     3-Benzamido, ureido and thioureidoimidazo[1,2-a]pyridine derivatives as potential antiviral agents.
     Chem. Pharm. Bull., 49: 1631-1635 (2001).
     


879. Vödrös, D., Thorstensson, R., Biberfeld, G., Schols, D., De Clercq, E. & Fenyö, E.M.
     Coreceptor usage of sequential isolates from cynomolgus monkeys experimentally infected with simian immunodeficiency virus (SIVsm).
     Virology, 291: 12-21 (2001).
     


880. Vödrös, D., Tscherning-Casper, C., Navea, L., Schols, D., De Clercq, E. & Fenyö, E.M.
     Quantitative evaluation of HIV-1 coreceptor use in the GHOST(3) cell assay.
     Virology, 291: 1-11 (2001).
     


881. Balzarini, J., Haller-Meier, F., De Clercq, E. & Meier, C.
     Antiviral activity of cyclosaligenyl prodrugs of acyclovir, carbovir and abacavir.
     Antiviral Chem. Chemother., 12: 301-306 (2001).
     


882. Harris, S.A., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis and antiviral evaluation of phosphoramidate derivatives of (E)-5-(2-bromovinyl)-2’-deoxyuridine.
     Antiviral Chem. Chemother., 12: 293-300 (2001).
     


883. Fontaine, E., Riva, C., Peeters, M., Schmit, J.-C., Delaporte, E., Van Laethem, K., Van Vaerenbergh, K., Snoeck, J., Van Wijngaerden, E., De Clercq, E., Van Ranst, M. & Vandamme, A.-M.
     Evaluation of two commercial kits for the detection of genotypic drug resistance on a panel of HIV type-1 subtypes A through J.
     JAIDS, 28: 254-258 (2001).
     


884. Lazrek, H.B., Taourirte, M., Oulih, T., Barascut, J.L., Imbach, J.L., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and anti-HIV activity of new modified 1,2,3-triazole acyclonucleosides.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1949-1960 (2001).
     


885. Tronchet, J.M.J., Kovacs, I., Dilda, P., Seman, M., Andrei, G., Snoeck, R., De Clerq, E. & Balzarini, J.
     Synthesis and anti-HIV activity of thymidine analogues bearing a 4’-cyanovinyl group and some derivatives thereof.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1927-1939 (2001).
     


886. De Clercq, E., Naesens, L., De Bolle, L., Schols, D., Zhang, Y. & Neyts, J.
     Antiviral agents active against human herpesviruses HHV-6, HHV-7, HHV-7 and HHV-8.
     Rev. Med. Virol., 11: 381-395 (2001).
     


887. Balzarini, J. & De Clercq, E.
     Rapid alternation of drug therapy is highly efficient in suppressing the emergence of mutant drug-resistant HIV strains in cell culture.
     AIDS Res. Hum. Retrovir., 17: 1625-1634 (2001).
     


888. Selvam, P., Chandramohan, M., De Clercq, E., Witvrouw, M. & Pannecouque, C.
     Synthesis and anti-HIV activity of 4-[(1,2-dihydro-2-oxo-3H-indol-3-ylidene)amino]-N(4,6-dimethyl-2-pyrimidinyl)-benzene sulfonamide and its derivatives.
     Eur. J. Pharm. Sci., 14: 313-316 (2001).
     


889. Kannan, A., De Clercq, E., Pannecouque, C., Witvrouw, M., Hartman, T.L., Turpin, J.A., Buckheit, R.W. Jr. & Cushman, M.
     Synthesis and anti-HIV activity of a bile acid analog of cosalane.
     Tetrahedron, 57: 9385-9391 (2001).
     


890. Hergueta, A.R., Fernández, F., López, C., Balzarini, J. & De Clercq, E.
     Novel carbocyclic nucleosides containing a cyclobutyl ring: adenosine analogues.
     Chem. Pharm. Bull., 49: 1174-1177 (2001).
     


891. De Clercq, E.
     New developments in anti-HIV chemotherapy.
     Curr. Med. Chem., 8: 1543-1572 (2001).
     


892. Golankiewicz, B., Ostrowski, T., Goslinski, T., Januszczyk, P., Zeidler, J., Baranowski, D. & De Clercq, E.
     Fluorescent tricyclic analogues of acyclovir and ganciclovir. A structure – antiviral activity study.
     J. Med. Chem., 44: 4284-4287 (2001).
     


893. Chamorro, C., Lobatón, E., Bonache, M.-C., De Clercq, E., Balzarini, J., Velázquez, S., San-Félix, A. & Camarasa, M.-J.
     Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
     Bioorg. Med. Chem. Lett., 11: 3085-3088 (2001).
     


894. Snoeck, R., Van Laethem, Y., De Clercq, E., De Maubeuge, J. & Clumeck, N.
     Treatment of a Bowenoid papulosis of the penis with local applications of cidofovir in a patient with acquired immunodeficiency syndrome.
     Arch. Intern. Med., 161: 2382-2384 (2001).
     


895. Del Corno, M., Liu, Q.-H., Schols, D., De Clercq, E., Gessani, S., Freedman, B.D. & Collman, R.G.
     HIV-1 gp120 and chemokine activation of Pyk2 and mitogen-activated protein kinases in primary macrophages mediated by calcium-dependent, pertussis toxin-insensitive chemokine receptor signaling.
     Blood, 98: 2909-2916 (2001).
     


896. De Clercq, E.
     Hamao Umezawa Memorial Award Lecture. An odyssey in the viral chemotherapy field.
     Int. J. Antimicrobial Agents, 18: 309-328 (2001).
     


897. Andrei, G., Snoeck, R., Schols, D. & De Clercq, E.
     Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells.
     Oncol. Res., 12: 397-408 (2001).
     


898. Moukha-Chafiq, O., Taha, M.L., Lazrek, H.B., Vasseur, J.J., Pannecouque, C., Witvrouw, M. & De Clercq, E.
     Synthesis and biological evaluation of some 4-substituted 1-[1-(4-hydroxybutyl)-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1811-1821 (2001).
     


899. Moukha-Chafiq, O., Taha, M.L., Lazrek, H.B., Pannecouque, C., Witvrouw, M., De Clercq, E., Barascut, J.L. & Imbach, J.L.
     Synthesis and biological activity of 4-substituted 1-[1-(2-hydroxyethoxy)methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1797-1810 (2001).
     


900. Hillenkamp, J., Reinhard, T., Ross, R.S., Böhringer, D., Cartsburg, O., Roggendorf, M., De Clercq, E., Godehardt, E. & Sundmacher, R.
     Topical treatment of acute adenoviral keratoconjunctivitis with 0.2% cidofovir and 1% cyclosporine.
     Arch. Ophthalmol., 119: 1487-1491 (2001).
     


901. Casimiro-Garcia, A., De Clercq, E., Pannecouque, C., Witvrouw, M., Loftus, T.L., Turpin, J.A., Buckheit, R.W. Jr., Fanwick, P.E. & Cushman, M.
     Synthesis and anti-HIV activity of cosalane analogues incorporating two dichlorodisalicylmethane pharmacophore fragments.
     Bioorg. Med. Chem., 9: 2827-2841 (2001).
     


902. Lewis, M. & De Clercq, E.
     Difluorinated carbaacyclonucleosides: synthesis and evaluation of antiviral activity.
     J. Chem. Res. (S), 2001: 311-312 (2001); J. Chem. Res. (M), 2001: 0844-0856 (2001).
     


903. Matthys, P., Hatse, S., Vermeire, K., Wuyts, A., Bridger, G., Henson, G.W., De Clercq, E., Billiau, A. & Schols, D.
     AMD3100, a potent and specific antagonist of the stromal cell-derived factor-1 chemokine receptor CXCR4, inhibits autoimmune joint inflammation in IFN- receptor-deficient mice..
     J. Immunol., 167, 4686-4692 (2001).
     


904. Debyser, Z., Cherepanov, P., Pluymers, W. & De Clercq, E.
     Assays for the evaluation of HIV-1 integrase inhibitors.
     In: “Methods in Molecular Biology”, vol. 160, “Nuclease Methods and Protocols”, C.H. Schein (ed.). Humana Press, Totowa, N.J., pp. 139-155 (2001).
     


905. Apers, S., Baronikova, S., Sindambiwe, J.B., Witvrouw, M., De Clercq, E., Vanden Berghe, D., Van Marck, E., Vlietinck, A. & Pieters, L.
     Antiviral, haemolytic and molluscicidal activities of triterpenoid saponins from Maesa lanceolata: establishment of structure-activity relationships.
     Planta Medica, 67: 528-532 (2001).
     


906. Carangio, A., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): Pd-catalysed synthesis of 5-aryl derivatives and their biological evaluation.
     Antiviral. Chem. Chemother., 12: 187-197 (2001).
     


907. Chimirri, A., Monforte, P., Rao, A., Zappalà, M., Monforte, A.M., De Sarro, G., Pannecouque, C., Witvrouw, M., Balzarini, J. & De Clercq, E.
     Synthesis, biological activity, pharmacokinetic properties and molecular modelling studies of novel 1H,3H-oxazolo[3,4-a]benzimidazoles: non-nucleoside HIV-1 reverse transcriptase inhibitors.
     Antiviral Chem. Chemother., 12: 169-174 (2001).
     


908. Zhang, Y., De Bolle, L., Aquaro, S., Van Lommel, A., De Clercq, E. & Schols, D.
     Productive infection of primary macrophages with human herpesvirus type 7.
     J. Virol., 75: 10511-10514 (2001).
     


909. Gorry, P.R., Bristol, G., Zack, J.A., Ritola, K., Swanstrom, R., Birch, C.J., Bell, J.E., Bannert, N., Crawford, K., Wang, H., Schols, D., De Clercq, E., Kunstman, K., Wolinsky, S.M. & Gabuzda, D.
     Macrophage tropism of human immunodeficiency virus type 1 isolates from brain and lymphoid tissues predicts neurotropism independent of coreceptor specificity.
     J. Virol., 75: 10073-10089 (2001).
     


910. Naesens, L. & De Clercq, E.
     Recent developments in herpesvirus therapy.
     Herpes, 8: 12-16 (2001).
     


911. Wirschung, J., Voss, J., Adiwidjaja, G., Balzarini, J. & De Clercq, E.
     Thiosugars. VIII. Preparation of new 4’-thio-L-lyxo pyrimidine nucleoside analogues.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1625-1645 (2001).
     


912. Pluymers, W., Cherepanov, P., De Clercq, E. & Debyser, Z.
     HIV-1 integration as a target for antiretroviral therapy: a review.
     Current Drug Targets – Infect. Disorders, 133-149 (2001).
     


913. De Clercq, E. & Schols, D.
     Inhibition of HIV infection by CXCR4 and CCR5 chemokine receptor antagonists.
     Antiviral Chem. Chemother., 12 (Suppl. 1): 19-31 (2001).
     


914. Jing, N., Marchand, C., Guan, Y., Liu J., Pallansch, L., Lackman-Smith, C., De Clercq, E. & Pommier, Y.
     Structure-activity of inhibition of HIV-1 integrase and virus replication by G-quartet oligonucleotides.
     DNA and Cell Biology, 20: 499-508 (2001).
     


915. Brancale, A., McGuigan, C., Algain, B., Savy, P., Benhida, R., Fourrey, J.-L., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic anti-VZV nucleosides: thieno analogues retain full antiviral activity.
     Bioorg. Med. Chem. Lett., 11: 2507-2510 (2001).
     


916. Ludovici, D.W., Kukla, M.J., Grous, P.G., Krishnan, S., Andries, K., de Béthune, M.-P., Azijn, H., Pauwels, R., De Clercq, E., Arnold, E. & Janssen, P.A.J.
     Evolution of anti-HIV drug candidates. Part 1: From -anilinophenylacetamide (-APA) to imidoyl thiourea (ITU).
     Bioorg. Med. Chem. Lett., 11: 2225-2228 (2001).
     


917. Rejman, D., Masojídková, M., De Clercq, E. & Rosenberg, I.
     2’-C-alkoxy and 2’-C-aryloxy derivatives of N-(2-phosphonomethoxyethyl)purines and
     –pyrimidines: synthesis and biological activity.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1497-1522 (2001).
     


918. Redwane, N., Lazrek, H.B., Barascut, J.L., Imbach, J.L., Balzarini, J., Witvrouw, M. & De Clercq, E.
     Synthesis and biological activities of (Z) and (E) -ethenyl acyclonucleosides.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 1439-1447 (2001).
     


919. Vlieghe, P., Clerc, T., Pannecouque, C., Witvrouw, M., De Clercq, E., Salles, J.-P. & Kraus, J.-L.
     New 3’-azido-3’-deoxythymidin-5’-yl O-(4-hydroxyalkyl or –alkenyl or –alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation.
     J. Med. Chem., 44: 3014-3021 (2001).
     


920. Stamatiou, G., Kolocouris, A., Kolocouris, N., Fytas, G., Foscolos, G.B., Neyts, J. & De Clercq, E.
     Novel 3-(2-adamantyl)pyrrolidines with potent activity against influenza A virus – identification of aminoadamantane derivatives bearing two pharmacophoric amine groups.
     Bioorg. Med. Chem. Lett., 11: 2137-2142 (2001).
     


921. Caamano, O., Figueira, M.J., Fernández, F., García, M.D., Nieto, M.I., De Clercq, E. & Balzarini, J.
     Synthesis and evaluation of antiviral activity of higher homologues of xylo-carbocyclic nucleosides.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 1137-1139 (2001).
     


922. López, C., Balo, C., Blanco, J.M., Fernández, F., De Clercq, E. & Balzarini, J.
     A cyclobutane carbonucleoside with marked selectivity against TK+ and TK- varicella-zoster virus.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 1133-1135 (2001).
     


923. Fernández, F., Hergueta, A.R., López, C., De Clercq, E. & Balzarini, J.
     Modified cyclobutane carbonucleosides: synthesis and evaluation of their antiviral activity.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 1129-1131 (2001).
     


924. Blewett, S., McGuigan, C., Barucki, H., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic furo pyrimidine nucleosides with aryloxyphenyl and halophenyl substituted side chains as potent and selective varicella-zoster virus inhibitors.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 1063-1066 (2001).
     


925. Takamatsu, S., Izawa, K., Maruyama, T., Katayama, S., Hirose, N. & De Clercq, E.
     Synthesis and in vitro antiviral activity evaluation of 9-(2-azido-2,3-dideoxy--D-threo-pentofuranosyl)adenine derivatives.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 1053-1057 (2001).
     


926. Renze, J., Plath, M., Ducho, C., Balzarini, J., De Clercq, E. & Meier, C.
     Benzyl-functionalized cycloSal-d4T monophosphates
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 931-934 (2001).
     


927. Srinivasan, S., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): effect of terminal unsaturation in the side-chain.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 763-766 (2001).
     


928. Wang, J., Froeyen, M., Hendrix, C., Andrei, G., Snoeck, R., Lescrinier, E., De Clercq, E. & Herdewijn, P.
     (D)- and (L)-cyclohexenyl-G, a new classof antiviral agents: synthesis, conformational analysis, molecular modeling, and biological activity.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 727-730 (2001).
     


929. Lobatón, E., Velázquez, S., San-Félix, A., De Clercq, E., Balzarini, J. & Camarasa, M.J.
     4”-H-TSAO-T, a novel prototype in the HIV-1 specific TSAO family.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 711-714 (2001).
     


930. Lobatón, E., Velázquez, S., Pérez-Pérez, M.J., Jimeno, M.L., San-Félix, A., De Clercq, E., Balzarini, J. & Camarasa, M.J.
     “Second generation” of TSAO compounds directed against HIV-1 TSAO-resistant strains.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 707-710 (2001).
     


931. Carangio, A., McGuigan, C., Cahard, D., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Synthesis and in vitro evaluation of novel anti-varicella-zoster virus (VZV) nucleosides.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 653-656 (2001).
     


932. Düzgünes, N., Simoes, S., Slepushkin, V., Pretzer, E., Rossi, J.J., De Clercq, E., Antao, V.P., Collins, M.L. & Pedroso de Lima, M.C.
     Enhanced inhibition of HIV-1 replication in macrophages by antisense oligonucleotides, ribozymes and acyclic nucleoside phosphonate analogs delivered in pH-sensitive liposomes.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides and Nucleic Acids, 20: 515-523 (2001).
     


933. McGuigan, C., Barucki, H., Carangio, A., Blewett, S., Srinivasan, S., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Novel aryl substituted bicyclic furo nucleosides as extremely potent and selective anti-VZV agents.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 287-296 (2001).
     


934. De Clercq, E, Andrei, G., Snoeck, R., De Bolle, L., Naesens, L., Degrève, B., Balzarini, J., Zhang, Y., Schols, D., Leyssen, P., Ying, C. & Neyts, J.
     Acyclic/carbocyclic guanosine analogues as anti-herpesvirus agents.
     Proceedings of the XIV International Round Table on “Nucleosides, Nucleotides and Their Biological Applications”, San Francisco, California, USA, 10-14 September 2000.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 271-285 (2001).
     


935. Chaouni-Benabdallah, A., Galtier, C., Allouchi, H., Kherbeche, A., Debouzy, J.-C., Teulade, J.-C., Chavignon, O., Witvrouw, M., Pannecouque, C., Balzarini, J., De Clercq, E., Enguehard, C. & Gueiffier, A.
     Synthesis of 3-nitrosoimidazo[1,2-a]pyridine derivatives as potential antiretroviral agents.
     Arch. Pharm. Pharm. Med. Chem., 334: 224-228 (2001).
     


936. Das, S.R., Schneller, S.W., Balzarini, J. & De Clercq, E.
     5’-Nor carbocyclic 5’-deoxy-5’-(isobutylthio)adenosine and a 2’,3’-dideoxy-2’,3’-didehydro derivative.
     Antiviral Chem. Chemother., 12: 119-124 (2001).
     


937. McGuigan, C., Brancale, A., Barucki, H., Srinivasan, S., Jones, G., Pathirana, R., Carangio, A., Blewett, S., Louni, G., Bidet, O., Jukes, A., Jarvis, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Furano pyrimidines as novel potent and selective anti-VZV agents.
     Antiviral Chem. Chemother., 12: 77-89 (2001).
     


938. Bijsterbosch, M.K., Ying, C., De Vrueh, R.L.A., De Clercq, E., Biessen, E.A.L., Neyts, J. & van Berkel, T.J.C.
     Carrier-mediated delivery improves the efficacy of 9-(2-phosphonylmethoxyethyl)adenine against hepatitis B virus.
     Mol. Pharmacol.,60: 521-527 (2001).
     


939. Guillerm, G., Guillerm, D., Vandenplas-Witkowki, C., Rogniaux, H., Carte, N., Leize, E., Van Dorsselaer, A., De Clercq, E. & Lambert, C.
     Synthesis, mechanism of action, and antiviral activity of a new series of covalent mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase.
     J. Med. Chem., 44: 2743-2752 (2001).
     


940. Pelemans, H., Esnouf, R., Min, K.-L., Parniak, M., De Clercq, E. & Balzarini, J.
     Mutations at amino acid positions 63, 189 and 396 of human immunodeficiency virus type 1 reverse transcriptase (RT) partially restore the DNA polymerase activity of a Trp229Tyr mutant RT.
     Virology, 287: 143-150 (2001).
     


941. Snoeck, R., Bossens, M., Parent, D., Delaere B., Degreef, H., Van Ranst, M., Noël, J.C., Wulfsohn, M., Rooney, J.F., Jaffe, H.S. & De Clercq, E.
     Phase II double-blind, placebo-controlled study of the safety and efficacy of cidofovir topical gel for the treatment of patients with human papillomavirus infection.
     Clin. Infect. Dis., 33: 597-602 (2001).
     


942. Baraldi, P.G., Balboni, G., Pavani, M.G., Spalluto, G., Aghazadeh, M., De Clercq, E., Balzarini, J., Bando, T., Sugiyama, H. & Romagnoli, R.
     Design, synthesis, DNA binding and biological evaluation of water-soluble hybrid molecules containing two pyrazole analogues of the alkylating cyclopropylpyrroloindole (CPI) subunit of the antitumor agent CC-1065 and polypyrrole minor groove binders.
     J. Med. Chem., 44: 2536-2543 (2001).
     


943. Geerinck, K., Lukito, G., Snoeck, R., De Vos, R., De Clercq, E., Vanrenterghem, Y., Degreef, H. & Maes, B.
     A case of human orf in an immunocompromised patient treated successfully with cidofovir cream.
     J. Med. Virol., 64: 543-549 (2001).
     


944. Barreca, M.L., Chimirri, A., De Luca, L., Monforte, A.-M., Monforte, P., Rao, A., Zappalà, M., Balzarini, J., De Clercq, E., Pannecouque, C. & Witvrouw, M.
     Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents.
     Bioorg. Med. Chem. Lett., 11: 1793-1796 (2001).
     


945. Andrei, G., Fiten, P., De Clercq, E., Snoeck, R. & Opdenakker, G.
     Evaluating phenotype and genotype of drug-resistant strains in herpesviruses.
     Mol. Biotechnol., 18: 155-167 (2001).
     


946. Griffon, J.-F., Mathé, C., Faraj, A., Aubertin, A.-M., De Clercq, E., Balzarini, J., Sommadossi, J.-P. & Gosselin, G.
     Stereospecific synthesis and biological evaluations of -L-pentofuranonucleoside derivatives of 5-fluorouracil and 5-fluorocytosine.
     Eur. J. Med. Chem., 36: 447-460 (2001).
     


947. Daelemans, D., De Clercq, E. & Vandamme, A.-M.
     A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors.
     J. Virol. Methods, 96: 183-188 (2001).
     


948. Struyf, S., Menten, P., Lenaerts, J.-P., Put, W., D’Haese, A., De Clercq, E., Schols, D., Proost, P. & Van Damme, J.
     Diverging binding capacities of natural LD78 isoforms of macrophage inflammatory protein-1 to the CC chemokine receptors 1, 3 and 5 affect their anti-HIV-1 activity and chemotactic potencies for neutrophils and eosinophils.
     Eur. J. Immunol., 31: 2170-2178 (2001).
     


949. Naimi, E., Wiebe, L.I., Balzarini, J., De Clercq, E. & Knaus, E.E.
     Synthesis of 1-(2-deoxy--D-ribofuranosyl)-2,4-difluoro-5-(2-halo-1-hydroxyethyl)-benzenes and related derivatives: “thymine replacement” analogs of deoxythymidine for evaluation as antiviral and anticancer agents.
     Drug Dev. Res., 52: 492-499 (2001).
     


950. Herdewijn, P. & De Clercq, E.
     The cyclohexene ring as bioisostere of a furanose ring: synthesis and antiviral activity of cyclohexenyl nucleosides.
     Bioorg. Med. Chem. Lett., 11: 1591-1597 (2001).
     


951. Liekens, S., Neyts, J., De Clercq E., Verbeken, E., Ribatti, D. & Presta, M.
     Inhibition of fibroblast growth factor-2-induced vascular tumor formation by the acyclic nucleoside phosphonate cidofovir.
     Cancer Res., 61: 5057-5064 (2001).
     


952. Bezzi, P., Domercq, M., Brambilla, L., Galli, R., Schols, D., De Clercq, E., Vescovi, A., Bagetta, G., Kollias, G., Meldolesi, J. & Volterra, A.
     CXCR4-activated astrocyte glutamate release via TNF: amplification by microglia triggers neurotoxicity.
     Nature Neuroscience, 4: 702-710 (2001).
     


953. Stephens, C.E., Felder, T.M., Sowell, J.W., Sr., Andrei, G., Balzarini, J., Snoeck, R. & De Clercq, E.
     Synthesis and antiviral/antitumor evaluation of 2-amino- and 2-carboxamido-3-arylsulfonylthiophenes and related compounds as a new class of diarylsulfones.
     Bioorg. Med. Chem. Lett., 9: 1123-1132 (2001).
     


954. Chamorro, C., Pérez-Pérez, M.-J., Rodríguez-Barrios, F., Gago, F., De Clercq, E., Balzarini, J., San-Félix, A. & Camarasa, M.-J.
     Exploring the role of the 5’-position of TSAO-T. Synthesis and anti-HIV evaluation of novel TSAO-T derivatives.
     Antiviral Res., 50: 207-222 (2001).
     


955. De Clercq, E.
     Antiviral drugs: current state of the art.
     J. Clin. Virol., 22: 73-89 (2001).
     


956. Mavel, S., Renou, J.L., Galtier, C., Snoeck, R., Andrei, G., Balzarini, J., De Clercq, E. & Gueffier, A.
     Synthesis of imidazo[1,2-a]pyridine derivatives as antiviral agents.
     Arzneimittel-Forsch. Drug Res., 51: 304-309 (2001).
     


957. Wirschung, J., Voss, J., Adiwidjaja, G., Balzarini, J. & De Clercq, E.
     Thiosugars. Part 9: Synthesis and biological evaluation of some 4’-thio-L-arabino nucleoside analogues.
     Bioorg. Med. Chem. Lett., 11: 1049-1051 (2001).
     


958. Koonsaeng, S., Verschraegen, C., Freedman, R., Bossens, M., Kudelka, A., Kavanagh, J., Suttisomwong, T., De Clercq, E. & Snoeck, R.
     Successful treatment of recurrent vulvar intraepithelial neoplasia resistant to interferon and isotretinoin with cidofovir.
     J. Med. Virol., 64: 195-198 (2001).
     


959. Van Vaerenbergh, K., Debaisieux, L., De Cabooter, N., Declercq, C., Desmet, K., Fransen, K., Maes, B., Marissens, D., Miller, K., Muyldermans, G., Sprecher, S., Stuyver, L., Vaira, D., Verhofstede, C., Zissis, G., Van Ranst, M., De Clercq, E., Desmyter, J. & Vandamme, A.-M.
     Prevalence of genotypic resistance among antiretroviral drug-naïve HIV-1-infected patients in Belgium.
     Antiviral Therapy, 6: 63-70 (2001).
     


960. Hatse, S., Princen, K., Gerlach, L.-O., Bridger, G., Henson, G., De Clercq, E., Schwartz, T.W. & Schols, D.
     Mutation of Asp171 and Asp262 of the chemokine receptor CXCR4 impairs its coreceptor function for human immunodeficiency virus-1 entry and abrogates the antagonistic activity of AMD3100.
     Mol. Pharmacol., 60: 164-173 (2001)
     


961. Vashishtha, S.C., Allen, T.M., Halleran, S., Szydlowski, J., Santos, C.L., De Clercq, E., Balzarini, J. & Dimmock, J.R.
     Cytotoxic and anticancer properties of some 4-aryl-3-arylcarbonyl-1-ethyl-4-piperidinols and related compounds.
     Die Pharmazie, 56: 390-393 (2001).
     


962. De Clercq, E., Andrei, G. & Snoeck, R.
     Cidofovir voor de behandeling van papillomateuze letsels.
     Tijdschr. Geneesk., 57: 695-702 (2001).
     


963. De Clercq, E.
     Vaccinia virus inhibitors as a paradigm for the chemotherapy of poxvirus infections.
     Clin. Microbiol. Rev., 14: 382-397 (2001).
     


964. Balzarini, J., Camarasa, M.-J., Pérez-Pérez, M.-J., San-Félix, A., Velázquez, S., Perno, C.-F., De Clercq, E., Anderson, J.N. & Karlsson, A.
     Exploitation of the low fidelity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase and the nucleotide composition bias in the HIV-1 genome to alter the drug-resistance development of HIV.
     J. Virol., 75: 5772-5777 (2001).
     


965. Manfredini, S., Baraldi, P.G., Durini, E., Porcu, L., Angusti, A., Vertuani, S., Solaroli, N., De Clercq, E., Karlsson, A. & Balzarini, J.
     Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors.
     Bioorg. Med. Chem. Lett., 11: 1329-1332 (2001).
     


966. Snoeck, R., Andrei, G. & De Clercq, E.
     Cidofovir in the treatment of HPV-associated lesions.
     Verh. K. Acad. Geneesk. Belg., 63: 93-122 (2001).
     


967. Mavromoustakos, T., Calogeropoulou, T., Koufaki, M., Kolocouris, A., Daliani, I., Demetzos, K., Meng, Z., Makriyannis, A., Balzarini, J. & De Clercq, E.
     Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers.
     J. Med. Chem., 44: 1702-1709 (2001).
     


968. Van Laethem, K., Witvrouw, M., Pannecouque, C., Van Remoortel, B., Schmit, J.-C., Esnouf, R., Kleim, J.-P., Balzarini, J., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
     Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype.
     AIDS, 15: 553-561 (2001).
     


969. De Clercq, E.
     New development in anti-HIV chemotherapy.
     Proceedings of the XVI International Symposium on Medicinal Chemistry, Bologna, Italy, 18-22 September 2000.
     Pure Appl. Chem., 73: 55-66 (2001).
     Il Farmaco, 56: 3-12 (2001).
     


970. Malkevitch, N., McDermott, D.H., Yi, Y., Grivel, J.-C., Schols, D., De Clercq, E., Murphy, P.M., Glushakova, S., Collman, R.G. & Margolis, L.
     Coreceptor choice and T cell depletion by R5, X4 and R5X4 HIV-1 variants in CCR5-deficient (CCR532) and normal human lymphoid tissue.
     Virology, 281: 239-247 (2001).
     


971. Aquaro, S., Menten, P., Struyf, S., Proost, P., Van Damme, J., De Clercq, E. & Schols, D.
     The LD78 isoform of MIP-1 is the most potent CC-chemokine in inhibiting CCR5-dependent human immunodeficiency virus type 1 replication in human macrophages.
     J. Virol., 75: 4402-4406 (2001).
     


972. Martin, R., Sterner, O., Alvarez, M., De Clercq, E., Minas, W. & Bailey, J.E.
     Collinone, a new recombinant angular polyketide antibiotic made by an engineered Streptomyces strain.
     J. Antibiotics, 54: 239-249 (2001).
     


973. Ballatore, C., McGuigan, C., De Clercq, E. & Balzarini, J.
     Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA.
     Bioorg. Med. Chem. Lett., 11: 1053-1056 (2001).
     


974. De Clercq, E.
     Molecular targets for antiviral agents.
     J. Pharmacol. Exp. Therapeutics, 297: 1-10 (2001).
     


975. Vandamme, A.-M. & De Clercq, E.
     Clinical usefulness of human immunodeficiency virus drug resistance monitoring.
     In: “Antiretroviral Therapy”. E. De Clercq (ed.). American Society for Microbiology, Washington DC, USA, pp. 243-277 (2001).
     


976. Balzarini, J., Esnouf, R. & De Clercq, E.
     Nonnucleoside reverse transcriptase inhibitors.
     In: “Antiretroviral Therapy”. E. De Clercq (ed.). American Society for Microbiology, Washington DC, USA, pp. 63-85 (2001).
     


977. Balzarini, J. & De Clercq, E.
     Nucleoside and nucleotide reverse transcriptase inhibitors.
     In: “Antiretroviral Therapy”. E. De Clercq (ed.). American Society for Microbiology, Washington DC, USA, pp. 31-62 (2001).
     


978. Schols, D. & De Clercq, E.
     Cellular receptors as targets for anti-human immunodeficiency virus agents.
     In: “Antiretroviral Therapy”. E. De Clercq (ed.). American Society for Microbiology, Washington DC, USA, pp. 11-30 (2001).
     


979. Asres, K., Bucar, F., Kartnig, T., Witvrouw, M., Pannecouque, C. & De Clercq, E.
     Antiviral activity against human immunodeficiency virus type-1 (HIV-1) and type 2 (HIV-2) of ethnobotanically selected Ethiopian medicinal plants.
     Phytother. Res., 15: 62-69 (2001).
     


980. Balzarini, J., Degrève, B., Zhu, C., Durini, E., Porcu, L., De Clercq, E., Karlsson, A. & Manfredini, S.
     2’-O-Acyl/alkyl-substituted arabinosyl nucleosides as inhibitors of human mitochondrial thymidine kinase.
     Biochem. Pharmacol., 61: 727-732 (2001).
     


981. Liekens, S., Verbeken, E., De Clercq, E. & Neyts, J.
     Potent inhibition of hemangiosarcoma development in mice by cidofovir.
     Int. J. Cancer, 92: 161-167 (2001).
     


982. Wang, Z.-X., Duan, W., Wiebe, L.I., Balzarini, J., De Clercq, E. & Knaus, E.E.
     Synthesis of 1-(2-deoxy--D-ribofuranosyl)-2,4-difluoro-5-substituted-benzenes: “thymine replacement” analogs of thymidine for evaluation as anticancer and antiviral agents.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 41-58 (2001).
     


983. Wang, Z.-X., Duan, W., Wiebe, L.I., Balzarini, J., De Clercq, E. & Knaus, E.E.
     Synthesis of 1-(2-deoxy--D-ribofuranosyl)-2,4-difluoro-5-substituted-benzene thymidine mimics, some related -anomers, and their evaluation as antiviral and anticancer agents.
     Nucleosides, Nucleotides & Nucleic Acids, 20: 11-40 (2001).
     


984. Varvaresou, A., Iakovou, K., Fillipatos, E., Souli, C., Calogeropoulou, T., Ioannidou, I., Kourounakis, A.P., Pannecouque, C., Witvrouw, M., Padalko, E., Neyts, J., De Clercq, E. & Tsotinis, A.
     Synthesis, antiretroviral and antioxidant evaluation of a series of new benzo[b]furan derivatives.
     Arzneim.-Forsch./Drug Res., 51: 156-162 (2001).
     


985. Vlieghe, P., Bihel, F., Clerc, T., Pannecouque, C., Witvrouw, M., De Clercq, E., Salles, J.-P., Chermann, J.-C. & Kraus, J.-L.
     New 3’-azido-3’-deoxythymidin-5’-yl O-(–hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation.
     J. Med. Chem., 44: 777-786 (2001).
     


986. Santhosh, K.C., Paul, G.C., De Clercq, E., Pannecouque, C., Witvrouw, M., Loftus, T.L., Turpin, J.A., Buckheit Jr., R.W. & Cushman, M.
     Correlation of anti-HIV activity with anion spacing in a series of cosalane analogs with extended polycarboxylate pharmacophores.
     J. Med. Chem., 44: 703-714 (2001).
     


987. Neyts, J. & De Clercq, E.
     The anti-herpesvirus activity of (1’S,2’R)-9-[[1’,2’-bis(hydroxymethyl)cycloprop-1’-yl]methyl]guanine is markedly potentiated by the immunosuppressive agent mycophenolate mofetil.
     Antiviral Res., 49: 121-127 (2001).
     


988. Neyts, J., Naesens, L., Ying, C., De Bolle, L. & De Clercq, E.
     Anti-herpesvirus activity of (1’S,2’R)-9-[[1’,2’-bis(hydroxymethyl)-cycloprop-1’-yl]methyl]guanine (A-5021) in vitro and in vivo.
     Antiviral Res., 49: 115-120 (2001).
     


989. Dimmock, J.R., Padmanilayam, M.P., Puthucode, R.N., Nazarali, A.J., Motaganahalli, N.L., Zello, G.A., Quail, J.W., Oloo, E.O., Kraatz, H.-B., Prisciak, J.S., Allen, T.M., Santos, C.L., Balzarini, J., De Clercq, E. & Manavathu.
     A conformational and structure-activity relationship study of cytotoxic 3,5-bis(arylidene)-4-piperidones and related N-acryloyl analogs.
     J. Med. Chem., 44: 586-593 (2001).
     


990. Pelemans, H., Aertsen, A., Van Laethem, K., Vandamme, A.-M., De Clercq, E., Pérez-Pérez, M.-J., San-Félix, A., Velázquez, S., Camarasa, M.-J. & Balzarini, J.
     Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.
     Virology, 280: 97-106 (2001).
     


991. Srinivasan, S., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
     Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): the effect of terminal unsaturation in the side chain.
     Bioorg. Med. Chem. Lett., 11: 391-393 (2001).
     


992. Degrève, B., Esnouf, R., De Clercq, E. & Balzarini, J.
     Mutation of 125 Gln to Asn selectively abolishes the thymidylate kinase activity of herpes simplex virus type 1 thymidine kinase.
     Mol. Pharmacol., 59: 285-293 (2001).
     


993. Van Valckenborgh, I., Wellens, W., De Boeck, K., Snoeck, R., De Clercq, E. & Feenstra, F.
     Systemic cidofovir in papillomatosis.
     Clin. Infect. Dis., 32: e62-e64 (2001).
     


994. Leyssen, P., Van Lommel, A., Drosten, C., Schmitz, H., De Clercq, E. & Neyts, J.
     A novel model for the study of the therapy of flavivirus infections using the Modoc virus.
     Virology, 279: 27-37 (2001).
     


995. Goebel, F.-D., Hemmer, R., Schmit, J.-C., Bogner, J.R., De Clercq, E., Witvrouw, M., Pannecouque, C., Valeyev, R., Vandevelde, M., Margery, H. & Tassignon, J.-P.
     Phase I/II dose escalation and randomized withdrawal study with add-on azodicarbo-namide in patients failing on current antiretroviral therapy.
     AIDS, 15: 33-45 (2001).
     


996. Liekens, S., De Clercq, E. & Neyts, J.
     Angiogenesis: regulators and clinical applications (Commentary).
     Biochem. Pharmacol., 61: 253-270 (2001).
     


997. Neyts, J. & De Clercq, E.
     Efficacy of 2-amino-7-(1,3-dihydroxy-2-propoxymethyl)purine for the treatment of vaccinia virus (orthopoxvirus) infections in mice.
     Antimicrob. Agents Chemother., 45: 84-87 (2001).
     


998. Naesens, L., De Bolle, L. & De Clercq, E.
     Antiviral activity of antiherpetic drugs in lymphoblast cells infected with human herpesvirus 6.
     Proceedings of the European Charcot Foundation Symposium on “Genes and Viruses in Multiple Sclerosis”, Venice, Italy, 28-30 October 1999. O.R. Hommes, H. Wekerle & M. Clanet (Eds.). Elsevier Science, pp. 241-250 (2001).
     



95 publications in the year 2000



999. Andrei, G., Fiten, P., De Clercq, E., Snoeck, R. & Opdenakker, G.
     Monitoring drug resistance for herpesviruses.
     In: “Methods in Molecular Medicine: Antiviral Methods and Protocols”, vol. 24. D. Kinchington & R.F. Schinazi (eds.). Humana Press Inc., Totowa, NJ, USA, pp. 151-169 (2000).
     


1000. Balzarini, J., Degrève, B., Esteban-Gamboa, A., Esnouf, R., De Clercq, E., Engelborghs, Y., Camarasa, M.-J. & Pérez-Pérez, M.-J.
      Kinetic analysis of novel multisubstrate analogue inhibitors of thymidine phosphorylase.
      FEBS Lett., 483: 181-185 (2000).
      


1001. Daelemans, D., De Clercq, E. & Vandamme, A.-M.
      Control of RNA initiation and elongation at the HIV LTR promoter.
      AIDS Rev., 2: 229-240 (2000).
      


1002. Verri, A., Focher, F., Duncombe, R.J., Basnak, I., Walker, R.T., Coe, P.L., De Clercq, E., Andrei, G., Snoeck, J., Balzarini, J. & Spadari, S.
      Anti-(herpes simplex virus) activity of 4’-thio-2’-deoxyuridines: a biochemical investigation for viral and cellular target enzymes.
      Biochem. J., 351: 319-326 (2000).
      


1003. Brancale, A., Srinivasan, S., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
      Synthesis and anti-varicella-zoster virus activity of some novel bicyclic nucleoside inhibitors: effect of enhanced aqueous solubility.
      Antiviral Chem. Chemother., 11: 383-393 (2000).
      


1004. McGuigan, C., Brancale, A., Barucki, H., Srinivasan, S., Jones, G., Pathirana, R., Blewett, S., Alvarez, R., Yarnold, C.J., Carangio, A., Velázquez, S., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
      Fluorescent bicyclic furo pyrimidine deoxynucleoside analogs as potent and selective inhibitors of VZV and potential future drugs for the treatment of chickenpox and shingles.
      Drugs of the Future, 25: 1151-1161 (2000).
      


1005. Dimmock, J.R., Kumar, P., Nazarali, A.J., Motaganahalli, N.L., Kowalchuk, T.P., Beazely, M.A., Quail, J.W., Oloo, E.O., Allen, T.M., Szydlowski, J., De Clercq, E. & Balzarini, J.
      Cytotoxic 2,6-bis(arylidene)cyclohexanones and related compounds.
      Eur. J. Med. Chem., 35: 967-977 (2000).
      


1006. Pandeya, S., Sriram, D., Nath, G. & De Clercq, E.
      Synthesis, antibacterial, antifungal and anti-HIV activities of norfloxacin Mannich bases.
      Eur. J. Med. Chem. 35: 249-255 (2000).
      


1007. Van Gelder, J., Shafiee, M., De Clercq, E., Penninckx, F., Van den Mooter, G., Kinget, R. & Augustijns, P.
      Species-dependent and site-specific intestinal metabolism of ester prodrugs.
      Int. J. Pharmaceutics, 205: 93-100 (2000).
      


1008. De Clercq, E.
      Guanosine analogues as anti-herpesvirus agents.
      Nucleosides, Nucleotides & Nucleic Acids, 19: 1531-1541 (2000).
      


1009. McGuigan, C., Barucki, H., Blewett, S., Carangio, A., Erichsen, J.T., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
      Highly potent and selective inhibition of varicella-zoster virus by bicyclic furopyrimidine nucleosides bearing an aryl side-chain.
      J. Med. Chem., 43: 4993-4997 (2000).
      


1010. Manolopoulos, V.G., Liekens, S., Koolwijk, P., Voets, T., Peters, E., Droogmans, G., Lelkes, P.I., De Clercq, E. & Nilius, B.
      Inhibition of angiogenesis by blockers of volume-regulated anion channels
      Gen. Pharmacol., 34: 107-116 (2000).
      


1011. Péloponèse Jr., J.-M., Grégoire, C., Opi, S., Esquieu, D., Sturgis, J., Lebrun, E., Meurs, E., Collette, Y., Olive, D., Aubertin, A.-M., Witvrouw, M., Pannecouque, C., De Clercq, E., Bailly, C., Lebreton, J. & Loret, E.P.
      1H-13C nuclear magnetic resonance assignment and structural characterization of HIV-1 Tat protein.
      C.R. Acad. Sci. Paris, Life Sci., 323: 883-894 (2000).
      


1012. Van Gelder, J., Deferme, S., Annaert, P., Naesens, L., De Clercq, E., Van den Mooter, G., Kinget, R. & Augustijns, P.
      Increased absorption of the antiviral ester prodrug tenofovir disoproxil in rat ileum by inhibiting its intestinal metabolism.
      Drug Metabolism & Disposition, 28: 1394-1396 (2000).
      


1013. Wang, Z.-X., Wiebe, L.I., Balzarini, J., De Clercq, E. & Knaus, E.E.
      Chiral synthesis of 4-[1-(2-deoxy--L-ribofuranosyl)] derivatives of 2-substituted 5-fluoroaniline: “cytosine replacement” analogues of deoxy--L-cytidine.
      J. Org. Chem., 65: 9214-9219 (2000).
      


1014. Raic-Malic, S., Svedruzic, D., Gazivoda, T., Marunovic, A., Hergold-Brundic, A., Nagl, A., Balzarini, J., De Clercq, E. & Mintas, M.
      Synthesis and antitumor activities of novel pyrimidine derivatives of 2,3-O,O-dibenzyl-6-deoxy-L-ascorbic acid and 4,5-didehydro-5,6-dideoxy-L-ascorbic acid.
      J. Med. Chem., 43: 4806-4811 (2000).
      


1015. Santhosh, K.C., De Clercq, E., Pannecouque, C., Witvrouw, M., Loftus, T.L., Turpin, J.A., Buckheit Jr., R.W. & Cushman, M.
      Anti-HIV activity of a series of cosalane amino acid conjugates.
      Bioorg. Med. Chem. Lett., 10: 2505-2508 (2000).
      


1016. McGuigan, C., Pathirana, R.N., Jones, G., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
      Anti-varicella-zoster virus bicyclic nucleosides: replacement of furo by pyrro base reduces antiviral potency.
      Antiviral Chem. Chemother., 11: 343-348 (2000).
      


1017. Moya, J., Pizarro, H., Jashés, M., De Clercq, E. & Sandino, A.M.
      In vivo effect of EICAR (5-ethynyl-1--ribofuranosylimidazole-carboxamide) on experimental infected rainbow trout (Oncorhynchus mykiss) and coho salmon (Oncorhynchus kisutch) fry with infectious pancreatic necrosis virus.
      Antiviral Res., 48: 125-130 (2000).
      


1018. Ying, C., De Clercq, E. & Neyts, J.
      Ribavirin and mycophenolic acid potentiate the activity of guanine- and diaminopurine-based nucleoside analogues against hepatitis B virus.
      Antiviral Res., 48: 117-123 (2000).
      


1019. Degrève, B., Esnouf, R., De Clercq, E. & Balzarini, J.
      Selective abolishment of pyrimidine nucleoside kinase activity of herpes simplex virus type 1 thymidine kinase by mutation of Alanine-167 to Tyrosine.
      Mol. Pharmacol., 58: 1326-1332 (2000).
      


1020. Baekelandt, V., Claeys, A., Cherepanov, P., De Clercq, E., De Strooper, B., Nuttin, B. & Debyser, Z.
      DNA-dependent protein kinase is not required for efficient lentivirus integration.
      J. Virol., 74: 11278-11285 (2000).
      


1021. Andrei, G., Snoeck, R. & De Clercq, E.
      Activity of D- and L-enantiomers of cyclohexenyl guanine against herpesviruses (Pointer).
      Int. Antiviral News, 8: 141-145 (2000).
      


1022. Paul, G.C., De Clercq, E., Pannecouque, C., Witvrouw, M., Loftus, T.L., Turpin, J.A., Buckheit Jr., R.W. & Cushman, M.
      Identification of optimal anion spacing for anti-HIV activity in a series of cosalane tetracarboxylates.
      Bioorg. Med. Chem. Lett., 10: 2149-2152 (2000).
      


1023. Wang, Z.-X., Duan, W., Wiebe, L.I., De Clercq, E., Balzarini, J. & Knaus, E.E.
      Synthesis of 1-[(2-hydroxyethoxy)methyl]- and 1-[(1,3-dihydroxy-2-propoxy)methyl]- derivatives of 5-substituted-2,4-difluorobenzene: unnatural acyclo thymidine mimics for evaluation as anticancer and antiviral agents.
      Nucleosides, Nucleotides & Nucleic Acids, 19: 1397-1411 (2000).
      


1024. Witvrouw, M., Fikkert, V., Pluymers, W., Matthews, B., Mardel, K., Schols, D., Raff, J., Debyser, Z., De Clercq, E., Holan, G. & Pannecouque, C.
      Polyanionic (i.e., polysulfonate) dendrimers can inhibit the replication of human immunodeficiency virus by interfering with both virus adsorption and later steps (reverse transcriptase/integrase) in the virus replicative cycle.
      Mol. Pharmacol., 58: 1100-1108 (2000).
      


1025. Balzarini, J., Aquaro, S., Knispel, T., Rampazzo, C., Bianchi, V., Perno, C.-F., De Clercq, E. & Meier, C.
      CycloSaligenyl-2’,3’-didehydro-2’,3’-dideoxythymidine monophosphate: efficient intracellular delivery of d4TMP.
      Mol. Pharmacol., 58: 928-935 (2000).
      


1026. Dimmock, J.R., Kandepu, N.M., Nazarali, A.J., Motaganahalli, N.L., Kowalchuk, T.P., Pugazhenthi, U., Prisciak, J.S., Quail, J.W., Allen, T.M., LeClerc, R., Santos, C.L., De Clercq, E. & Balzarini, J.
      Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)-phenylmethylene]cyclohexanones and related compounds.
      J. Med. Chem., 43: 3933-3940 (2000).
      


1027. Degrève, B., De Clercq, E. & Balzarini, J.
      Selection of HSV-1 TK gene-transfected murine mammary carcinoma cells resistant to (E)-5-(2-bromovinyl)-2’-deoxyuridine (BVDU) and ganciclovir (GCV).
      Gene Therapy, 7: 1543-1552 (2000).
      


1028. Balzarini, J., Zhu, C., De Clercq, E., Pérez-Pérez, M.-J., Chamorro, C., Camarasa, M.-J. & Karlsson, A.
      Novel ribofuranosylnucleoside lead compounds for potent and selective inhibitors of mitochondrial thymidine kinase-2.
      Biochem. J., 351: 167-171 (2000).
      


1029. Wang, Z.-X., Wiebe, L.I., De Clercq, E., Balzarini, J. & Knaus, E.E.
      Syntheses of 4-[1-(2-deoxy--D-ribofuranosyl)]-derivatives of 2-substituted-5-fluoro-aniline: “cytosine replacement” analogs of deoxycytidine for evaluation as anticancer and antihuman immunodeficiency virus (anti-HIV) agents.
      Can. J. Chem., 78: 1081-1088 (2000).
      


1030. Pluymers, W., Neamati, N., Pannecouque, C., Fikkert, V., Marchand, C., Burke, T.R. Jr., Pommier, Y., Schols, D., De Clercq, E., Debyser, Z. & Witvrouw, M.
      Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters.
      Mol. Pharmacol., 58: 641-648 (2000).
      


1031. San-Félix, A., Chamorro, C., Pérez-Pérez, M.J., Velázquez, S., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Synthesis of novel 5’-substituted TSAO-T analogues with anti-HIV-1 activity.
      J. Carbohydrate Chem;, 19: 635-640 (2000).
      


1032. Camarasa, M.J., San-Félix, A., Pérez-Pérez, M., Velázquez, S., Alvarez, R., Chamorro, C., Jimeno, M.L., Pérez, C., Gago, F., De Clercq, E. & Balzarini, J.
      HIV-1 specific reverse transcriptase inhibitors: why are TSAO-nucleosides so unique ?
      J. Carbohydrate Chem., 19: 451-469 (2000).
      


1033. Martinez, A., Gil, C., Perez, C., Castro, A., Prieto, C., Otero, J., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Nonnucleoside human cytomegalovirus inhibitors: synthesis and antiviral evaluation of (chlorophenylmethyl)benzothiadiazine dioxide derivatives.
      J. Med. Chem., 43: 3267-3273 (2000).
      


1034. Balayiannis, G., Karigiannis, G., Gatos, P., Papaioannou, D. & De Clercq, E.
      Total syntheses of novel dideoxynucleoside analogues using chiral amino acids.
      Tetrahedron Lett., 41: 6191-6194 (2000).
      


1035. De Clercq, E.
      Current lead natural products for the chemotherapy of human immunodeficiency virus (HIV) infection.
      Med. Res. Rev., 20: 323-349 (2000).
      


1036. De Clercq, E.
      Novel compounds in preclinical/early clinical development for the treatment of HIV infections.
      Rev. Med. Virol., 10: 255-277 (2000).
      


1037. De Clercq, E.
      Reverse transcriptase inhibitors as anti-HIV drugs.
      In: “Antivirals against AIDS”, R.E. Unger, J. Kreuter & H. Rübsamen-Waigmann (eds.). Marcel Dekker, New York, pp. 107-150 (2000).
      


1038. De Clercq, E.
      Structures et activités des inhibiteurs non-nucléosidiques de la transcriptase inverse du VIH (INNTI).
      Méd. Mal. Infect., 30: 421-430 (2000).
      


1039. Snoeck, R., Andrei, G. & De Clercq, E.
      Novel agents for the therapy of varicella-zoster virus infections.
      Exp. Opin. Invest. Drugs, 9: 1743-1751 (2000).
      


1040. Wirsching, J., Voss, J., Balzarini, J. & De Clercq, E.
      Thiosugars. Part 5: synthesis and biological activity of 1-(4-thio-L-arabinofuranosyl)-5-halopyrimidine nucleosides.
      Bioorg. Med. Chem. Lett., 10: 1339-1341 (2000).
      


1041. Siddiqui, A., McGuigan, C., Ballatore, C., Srinivasan, S., De Clercq, E. & Balzarini, J.
      Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs.
      Bioorg. Med. Chem. Lett., 10: 381-384 (2000).
      


1042. Annaert, P., Tukker, J.J., Van Gelder, J., Naesens, L., De Clercq, E., Van den Mooter, G., Kinget, R. & Augustijns, P.
      In vitro, ex vivo, and in situ intestinal absorption characteristics of the antiviral ester prodrug adefovir dipivoxil.
      J. Pharm. Res., 89: 1054-1062 (2000).
      


1043. Cherepanov, P., Pluymers, W., Claeys, A., Proost, P., De Clercq, E. & Debyser, Z.
      High-level expression of active HIV-1 integrase from a synthetic gene in human cells.
      FASEB J., 14: 1389-1399 (2000).
      


1044. Van Vaerenbergh, K., Van Laethem, K., Albert, J., Boucher, C., Clotet, B., Floridia, M., Gerstoft, J., Hejdeman, B., Nielsen, C., Pannecouque, C., Perrin, L., Pirillo, M.F., Ruiz, L., Schmit, J.C., Schneider, F., Schoolmeester, A., Schuurman, R., Stellbrink, H.J., Stuyver, L., Van Lunzen, J., Van Remoortel, B., Van Wijngaerden, E., Vella, S., Witvrouw, M., Yerly, S., De Clercq, E., Desmyter, J. & Vandamme, A.-M.
      Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.
      Antimicrob. Agents Chemother, 44: 2109-2117 (2000).
      


1045. Al-Masoudi, N.A., Al-Soud, Y.A., Eherman, M. & De Clercq, E.
      Synthesis of acyclic 6,7-dihaloquinolone nucleoside analogues as potential antibacterial and antiviral agents.
      Bioorg. Med. Chem., 8: 1407-1413 (2000).
      


1046. Brancale, A., McGuigan, C., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
      Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): the effect of a terminal halogen substitution in the side chain.
      Bioorg. Med. Chem. Lett., 10: 1215-1217 (2000).
      


1047. Lazarini, F., Casanova, P., Tham, T.N., De Clercq, E., Arenzana-Seisdedos, F., Baleux, F. & Dubois-Dalcq, M.
      Differential signalling of the chemokine receptor CXCR4 by stromal cell-derived factor 1 and the HIV glycoprotein in rat neurons and astrocytes.
      Eur. J. Neurosci., 12: 117-125 (2000).
      


1048. De Clercq, E.
      A crusade for drugs to conquer viruses.
      In: “Many Faces, Many Microbes: Personal Reflections in Microbiology”, R.M. Atlas (ed.). ASM Press, Washington DC, pp. 164-170 (2000).
      


1049. Wijnholds, J., Mol, C.A.A.M., van Deemter, L., de Haas, M., Scheffer, G.L., Baas, F., Beijnen, J.H., Scheper, R.J., Hatse, S., De Clercq, E., Balzarini, J. & Borst, P.
      Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogues.
      Proc. Natl. Acad. Sci. USA, 97: 7476-7481 (2000).
      


1050. Martinez, A., Esteban, A.I., Castro, A., Gil, C., Conde, S., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Thienothiadiazine 2,2-dioxide acyclonucleosides: synthesis and antiviral activity.
      Antiviral Chem. Chemother., 11: 221-230 (2000).
      


1051. Pandeya, S.N., Sriram, D., Nath, G. & De Clercq, E.
      Synthesis, antibacterial, antifungal and anti-HIV evaluation of Schiff and Mannich bases of isatin and its derivatives with triazole.
      Arzneim.-Forsch./Drug Res., 50: 55-59 (2000).
      


1052. Van Laethem, K., Schmit, J.-C., Pelemans, H., Balzarini, J., Witvrouw, M., Pérez-Pérez, M.J., Camarasa, M.-J., Esnouf, R.M., Aquaro, S., Cenci, A., Perno, C.-F., Hermans, P., Sprecher, S., Ruiz, L., Clotet, B., Van Wijngaerden, E., Van Ranst, M., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Presence of 2’,5’-bis-O-(tert-butyldimethylsilyl)-3’-spiro-5”-(4”-amino-1”,2”-oxathiole-2”,2”-doxide) (TSAO)-resistant virus strains in TSAO-inexperienced patients.
      AIDS Res. Hum. Retrovir., 16: 825-833 (2000).
      


1053. Jonckheere, H., De Clercq, E. & Anné, J.
      Fidelity analysis of HIV-1 reverse transcriptase mutants with an altered amino-acid sequence at residues Leu74, Glu89, Tyr115, Tyr183 and Met184
      Eur. J. Biochem., 267: 2658-2665 (2000).
      


1054. Neyts, J., Andrei, G., Snoeck, R., Meerbach, A. & De Clercq, E.
      Methods in Anti-HCMV research.
      In: “Methods in Molecular Medicine”, vol. 33. “Cytomegalovirus Protocols”, J. Sinclair (ed.). Humana Press, Totowa, N.J., pp. 129-152 (2000).
      


1055. Liu, Q.-H., Williams, D.A., McManus, C., Baribaud, F., Doms, R.W., Schols, D., De Clercq, E., Kotlikoff, M.I., Collman, R.G. & Freedman, B.D.
      HIV-1 gp120 and chemokines activate ion channels in primary macrophages through CCR5 and CXCR4 stimulation.
      Proc. Natl. Acad. Sci. USA, 97: 4832-4837 (2000).
      


1056. De Clercq, E.
      CXCR4 and CCR5 chemokine receptor antagonists as anti-HIV agents, with special emphasis on the CXCR4 antagonist AMD-3100.
      Curr. Opin. Anti-Infect. Invest. Drugs, 2: 226-236 (2000).
      


1057. Witvrouw, M., Pannecouque, C., Desmyter, J., De Clercq, E. & Andries, K.
      In vitro evaluation of the effect of temporary removal of HIV drug pressure.
      Antiviral Res., 46: 215-221 (2000).
      


1058. Estrada, E., Uriarte, E., Montero, A., Teijeira, M., Santana, L. & De Clercq, E.
      A novel approach for the virtual screening and rational design of anticancer compounds.
      J. Med. Chem., 43: 1975-1985 (2000).
      


1059. De Clercq, E.
      The molecular targets for HIV inhibitors (Pointer).
      Int. Antiviral News, 8: 53-56 (2000).
      


1060. De Clercq, E.
      Identification of the real molecular target for HIV inhibitors (Letter).
      Trends Pharmacol. Sci., 21: 167-168 (2000).
      


1061. Wyde, P.R., Moore-Poveda, D.K., De Clercq, E., Neyts, J., Matsuda, A., Guzman, E. & Gilbert, B.E.
      Use of cotton rats to evaluate the efficacy of antivirals in treatment of measles virus infections.
      Antimicrob. Agents Chemother., 44: 1146-1152 (2000).
      


1062. Pelemans, H., Esnouf, R., De Clercq, E. & Balzarini, J.
      Mutational analysis of Trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors.
      Mol. Pharmacol., 57: 954-960 (2000).
      


1063. De Clercq, E.
      Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists. Minireview.
      Mol. Pharmacol., 57: 833-839 (2000).
      


1064. McGuigan, C., Bidois, L., Hiouni, A., Ballatore, C., De Clercq, E. & Balzarini, J.
      Phosphoramidate derivatives of stavudine as inhibitors of HIV: unnatural amino acids may substitute for alanine.
      Antiviral Chem. Chemother., 11: 111-116 (2000).
      


1065. Pierra, C., Imbach, J.-L., De Clercq, E., Balzarini, J., Van Aerschot, A., Herdewijn, P., Faraj, A., Loi, A.G., Sommadossi, J.-P. & Gosselin, G.
      Synthesis and antiviral evaluation of some -L-2’,3’-dideoxy-5-chloropyrimidine nucleosides and pronucleotides.
      Antiviral Res., 45: 169-183 (2000).
      


1066. Andrei, G., Snoeck, R., Neyts, J., Sandvold, M.L., Myhren, F. & De Clercq, E.
      Antiviral activity of ganciclovir elaidic acid ester against herpesviruses
      Antiviral Res., 45: 157-167 (2000).
      


1067. Van Vaerenbergh, K., Van Laethem, K., Van Wijngaerden, E., Schmit, J.-C., Schneider, F., Ruiz, L., Clotet, B., Verhofstede, C., Van Wanzeele, F., Muyldermans, G., Simons, P., Stuyver, L., Hermans, P., Evans, C., De Clercq, E., Desmyter, J. & Vandamme, A.-M.
      Baseline HIV type 1 genotypic resistance to a newly added nucleoside analog is predictive of virologic failure of the new therapy.
      AIDS Res. Hum. Retrovir., 16: 529-537 (2000).
      


1068. Balzarini, J., De Clercq, E., Carbonez, A., Burt, V. & Kleim, J.-P.
      Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors.
      AIDS Res. Hum. Retrovir., 16: 517-528 (2000).
      


1069. Ying, C., De Clercq, E., Nicholson, W., Furman, P. & Neyts, J.
      Inhibition of the replication of the DNA polymerase M550V mutation variant of human hepatitis B virus by adefovir, tenofovir, L-FMAU, DAPD, penciclovir and lobucavir.
      J. Viral Hepatitis, 7: 161-165 (2000).
      


1070. Ying, C., De Clercq, E. & Neyts, J.
      Lamivudine, adefovir and tenofovir exhibit long-lasting anti-hepatitis B virus activity in cell culture.
      J. Viral Hepatitis, 7: 79-83 (2000).
      


1071. Balzarini, J., Degrève, B., Hatse, S., De Clercq, E., Breuer, M., Johansson, M., Huybrechts, R. & Karlsson, A.
      The multifunctional deoxynucleoside kinase of insect cells is a target for the development of new insecticides.
      Mol. Pharmacol., 57: 811-819 (2000).
      


1072. Tronchet, J.M.J., Kovacs, I., Seman, M., Dilda, P., De Clercq, E. & Balzarini, J.
      Highly stereoselective synthesis and biological properties of nucleoside analogues bearing a spiro inserted oxirane ring.
      Nucleosides, Nucleotides & Nucleic Acids, 19: 775-794 (2000).
      


1073. Neyts, J., Kristmundsdóttir, T., De Clercq, E. & Thormar, H.
      Hydrogels containing monocaprin prevent intravaginal and intracutaneous infections with HSV-2 in mice: impact on the search for vaginal microbicides.
      J. Med. Virol., 61: 107-110 (2000).
      


1074. Wnuk, S.F., Valdez, C.A., Khan, J., Moutinho, P., Robins, M.J., Yang, X., Borchardt, R.T., Balzarini, J. & De Clercq, E.
      Doubly homologated dihalovinyl and acetylene analogues of adenosine. Synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects.
      J. Med. Chem., 43: 1180-1186 (2000).
      


1075. Leyssen, P., De Clercq, E. & Neyts, J.
      Perspectives for the treatment of infections with Flaviviridae.
      Clin. Microbiol. Rev., 13: 67-82 (2000).
      


1076. Esteban-Gamboa, A., Balzarini, J., Esnouf, R., De Clercq, E., Camarasa, M.-J. & Pérez-Pérez, M.-J.
      Design, synthesis and enzymatic evaluation of multisubstrate analogue inhibitors of Escherichia coli thymidine phosphorylase.
      J. Med. Chem., 43: 971-983 (2000).
      


1077. Witvrouw, M., Weigold, H., Pannecouque, C., Schols, D., De Clercq, E. & Holan, G.
      Potent anti-HIV (type 1 and type 2) activity of polyoxometalates: structure-activity-relationship and mechanism of action.
      J. Med. Chem., 43: 778-783 (2000).
      


1078. Jonckheere, H., Anné, J. & De Clercq, E.
      The HIV-1 reverse transcription (RT) process as target for RT inhibitors.
      Med. Res. Rev., 20: 129-154 (2000).
      


1079. Van Laethem, K., Witvrouw, M., Balzarini, J., Schmit, J.-C., Sprecher, S., Hermans, P., Leal, M., Harrer, T., Ruiz, L., Clotet, B., Van Ranst, M., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Patient HIV-1 strains carrying the multiple nucleoside resistance mutations are cross-resistant to abacavir.
      AIDS, 14: 469-471 (2000).
      


1080. Teran, C., Santana, L., Teijeira, M., Uriarte, E. & De Clercq, E.
      Design, synthesis, conformational analysis and biological activities of purine-based 1,2-di-substituted carbocyclic nucleosides.
      Chem. Pharm. Bull. 48: 293-295 (2000).
      


1081. Wang, J., Froeyen, M., Hendrix, C., Andrei, G., Snoeck, R., De Clercq, E. & Herdewijn, P.
      The cyclohexene ring system as a furanose mimic: synthesis and antiviral activity of both enantiomers of cyclohexenylguanine.
      J. Med. Chem., 43: 736-745 (2000).
      


1082. Jing, N., De Clercq, E., Rando, R.F., Pallansch, L., Lackman-Smith, C., Lee, S. & Hogan, M.E.
      Stability-activity relationships of a family of G-tetrad forming oligonucleotides as potent HIV inhibitors.
      J. Biol. Chem., 275: 3421-3430 (2000).
      


1083. Zhang, Y., Hatse, S., De Clercq, E. & Schols, D.
      CXC-chemokine receptor 4 is not a coreceptor for human herpesvirus type 7 entry into CD4+ T cells.
      J. Virol., 74: 2011-2016 (2000).
      


1084. Andrei, G., Snoeck, R., De Clercq, E., Esnouf, R., Fiten, P. & Opdenakker, G.
      Resistance of herpes simplex virus type 1 against different phosphonylmethoxyalkyl derivatives of purines and pyrimidines due to specific mutations in the viral DNA polymerase gene.
      J. Gen. Virol., 81: 639-648 (2000).
      


1085. Casimiro-Garcia, A., De Clercq, E., Pannecouque, C., Witvrouw, M., Stup, T.L., Turpin, J.A., Buckheit, R.W. Jr. & Cushman, M.
      Synthesis and anti-HIV activity of cosalane analogues incorporating nitrogen in the linker chain.
      Bioorg. Med. Chem., 8: 191-200 (2000).
      


1086. Jashés, M., Mlynarz, G., De Clercq, E. & Sandino, A.M.
      Inhibitory effects of of EICAR on infectious pancreatic necrosis virus replication.
      Antiviral Res., 45: 9-17 (2000).
      


1087. Chamorro, C., De Clercq, E., Balzarini, J., Camarasa, M.-J. & San-Félix, A.
      TSAO-T analogues bearing amino acids at position N-3 of thymine: synthesis and anti-human immunodeficiency virus activity.
      Antiviral Chem. Chemother., 11: 61-69 (2000).
      


1088. Aquaro, S., Wedgwood, O., Yarnold, C., Cahard, D., Pathinara, R., McGuigan, C., Calio, R., De Clercq, E., Balzarini, J. & Perno, C.F.
      Activities of masked 2’-3’-dideoxynucleoside monophosphate derivatives against human immunodeficiency virus in resting macrophages.
      Antimicrob. Agents Chemother., 44: 173-177 (2000).
      


1089. Blanco, J., Barretina, J., Henson, G., Bridger, G., De Clercq, E., Clotet, B. & Esté, J.A.
      The CXCR4 antagonist AMD3100 efficiently inhibits cell-surface-expressed human immunodeficiency virus type 1 envelope-induced apoptosis.
      Antimicrob. Agents Chemother., 44: 51-56 (2000).
      


1090. Schramm, B., Penn, M.L., Speck, R.F., Chan, S.Y., De Clercq, E., Schols, D., Connor, R.I. & Goldsmith, M.A.
      Viral entry through CXCR4 is a pathogenic factor and therapeutic target in human immunodeficiency virus type 1 disease.
      J. Virol., 74: 184-192 (2000).
      


1091. Daelemans, D., Schols, D., Witvrouw, M., Pannecouque, C., Hatse, S., Van Dooren, S., Hamy, F., Klimkait, T., De Clercq, E. & Vandamme, A.-M.
      A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
      Mol. Pharmacol., 57: 116-124 (2000).
      


1092. Snoeck, R., Noel, J.C., Muller, C., De Clercq, E. & Bossens, M.
      Cidofovir, a new approach for the treatment of cervix intraepithelial neoplasia grade III (CIN III).
      J. Med. Virol., 60: 205-209 (2000).
      


1093. Vandamme, A.-M., Witvrouw, M., Pannecouque, C., Balzarini, J., Van Laethem, K., Schmit, J.-C., Desmyter, J. & De Clercq, E.
      Evaluating clinical isolates for their phenotypic and genotypic resistance against anti-HIV drugs.
      In: “Methods in Molecular Medicine: Antiviral Methods and Protocols”, vol. 24. D. Kinchington & R.F. Schinazi (eds.). Humana Press Inc., Totowa, NJ, USA, pp. 223-258 (2000).
      



106 publications in the year 1999



1094. Vandamme, A.-M., Van Laethem, K. & De Clercq, E.
      Managing resistance to anti-HIV drugs. An important consideration for effective disease management.
      Drugs, 57: 337-361 (1999).
      


1095. Snoeck, R., Andrei, G. & De Clercq, E.
      Current pharmacological approaches to the therapy of varicella-zoster virus infections: a guide to treatment.
      Drugs, 57: 187-206 (1999).
      


1096. Lhassani, M., Chavignon, O., Chezal, J.-M., Teulade, J.-C., Chapat, J.-P., Snoeck, R., Andrei, G., Balzarini, J., De Clercq, E. & Gueiffier, A.
      Synthesis and antiviral activity of imidazo[1,2-apyridines.
      Eur. J. Med. Chem., 34: 271-274 (1999).
      


1097. De Clercq, E.
      The emerging role of fusion inhibitors in HIV infection.
      Drugs in R&D, 2: 321-331 (1999).
      


1098. Pandeya, S.N., Sriram, D., Nath, G. & De Clercq, E.
      Synthesis and antimicrobial activity of Schiff and Mannich bases of isatin and its derivatives with pyrimidine.
      Il Farmaco, 54: 624-628 (1999).
      


1099. Pandeya, S.N., Sriram, D., Nath, G. & De Clercq, E.
      Synthesis, antibacterial, antifungal and anti-HIV evaluation of Schiff and Mannich bases of isatin derivatives with 3-amino-2-methylmercapto quinazolin-4(3H)-one.
      Pharm. Acta Helvetiae, 74: 11-17 (1999).
      


1100. Breslin, H.J., Kukla, M.J., Kromis, T., Cullis, H., De Knaep, F., Pauwels, R., Andries, K., De Clercq, E., Janssen, M.A.C. & Janssen, P.A.J.
      Synthesis and anti-HIV activity of 1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one (TBO) derivatives. Truncated 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-ones (TIBO) analogues.
      Bioorg. Med. Chem., 7: 2427-2436 (1999).
      


1101. Afouna, M.I., Mehta, S.C., Ghanem, A.-H., Higuchi, W.I., Kern, E.R., De Clercq, E. & El-Shattawy, H.H.
      Influence of the treatment protocol upon the in vivo efficacy of cidofovir (HPMPC) and of acyclovir (ACV) formulations in topical treatment of cutaneous HSV-1 infection in hairless mice.
      J. Pharm. Sci., 88: 530-534 (1999).
      


1102. Gong, Z.J., De Meyer, S., Clarysse, C., Verslype, C., Neyts, J., De Clercq, E. & Yap, S.H.
      Mycophenolic acid, an immunosuppressive agent, inhibits HBV replication in vitro.
      J. Viral Hepatitis, 6: 229-236 (1999).
      


1103. Pandeya, S.N., Yogeeswari, P., Sriram, D., De Clercq, E., Pannecouque, C. & Witvrouw, M.
      Synthesis and screening for anti-HIV activity of some N-Mannich bases of isatin derivatives.
      Chemotherapy, 45: 192-196 (1999).
      


1104. Terán, C., Santana, L., Teijeira, M., Uriarte, E., Balzarini, J. & De Clercq, E.
      Synthesis and chemotherapeutic activity of a carbocyclic analogue of tegafur.
      Pharmazie, 53: 644 (1999).
      


1105. Blanco, J., Jacotot, E., Cabrera, C., Cardona, A., Clotet, B., De Clercq, E. & Esté, J.A.
      The implication of the chemokine CXCR4 in HIV-1 envelope-induced apoptosis is independent of the G-protein-mediated signaling.
      AIDS, 13: 909-917 (1999).
      


1106. Kundu, N.G., Mahanty, J.S., Chowdhury, C., Dasgupta, S.K., Das, B., Spears, C.P., Balzarini, J. & De Clercq, E.
      5-(Acylethynyl)uracils, 5-(acylethynyl)-2’-deoxyuridines and 5-(acetylethynyl)-1-(2-hydroxyethoxy)methyluracils. Their synthesis, antiviral and cytotoxic activities.
      Eur. J. Med. Chem., 34: 389-398 (1999).
      


1107. De Bruyne, T., Pieters, L., Witvrouw, M., De Clercq, E., Vanden Berghe, D. & Vlietinck, A.J.
      Biological evaluation of proanthocyanidin dimers and related polyphenols.
      J. Natural Products, 62: 954-958 (1999).
      


1108. Hibbitts, S., Reeves, J.D., Simmons, G., Gray, P.W., Epstein, L.G., Schols, D., De Clercq, E., Wells, T.N.C., Proudfoot, A.E.I. & Clapham, P.R..
      Coreceptor ligand inhibition of fetal brain cell infection by HIV type 1.
      AIDS Res. Hum. Retrovir., 15: 989-1000 (1999).
      


1109. Degrève, B., De Clercq, E., Karlsson, A. & Balzarini, J.
      Efficacy of antiherpetic drugs in combined gene/chemotherapy of cancer is not affected by a specific nuclear or cytoplasmic compartmentation of herpes thymidine kinases.
      Gene Ther. Mol. Biol., 3: 123-131 (1999).
      


1110. Kolocouris, A., Tataridis, D., Fytas, G., Mavromoustakos, T., Foscolos, G.B., Kolocouris, N. & De Clercq, E.
      Synthesis of 2-(2-adamantyl)piperidines and structural anti-influenza virus A activity relationship study using a combination of NMR spectroscopy and molecular modelling.
      Bioorg. Med. Chem. Lett., 9: 3465-3470 (1999).
      


1111. Swart, P.J., Harmsen, M.C., Kuipers, M.E., van Dijk, A.A., van der Strate, B.W.A., Van Berkel, P.H.C., Nuijens, J.H., Smit, C., Witvrouw, M., D. De Clercq, E., de Béthune, M.-P., Pauwels, R. & Meijer, D.K.F.
      Charge modification of plasma and milk proteins results in antiviral active compounds.
      J. Peptide Sci., 5: 563-576 (1999).
      


1112. Pandeya, S.N., Sriram, D., Nath, G. & De Clercq, E.
      Synthesis, antibacterial, antifungal and anti-HIV activity of Schiff and Mannich bases of isatin with N-[6-chlorobenzothiazol-2-yl]thiosemicarbazide.
      Indian J. Pharm. Sci., 61: 358-361 (1999).
      


1113. Pandeya, S.N., Sriram, D., Nath, G. & De Clercq, E.
      Synthesis, antibacterial, antifungal and anti-HIV activities of Schiff and Mannich bases derived from isatin derivatives and N-[4-(4’-chlorophenyl)thiazol-2-yl]thiosemicarbazide.
      Eur. J. Pharm. Sci., 9: 25-31 (1999).
      


1114. Glushakova, S., Yi, Y., Grivel, J.-C., Singh, A., Schols, D., De Clercq, E., Collman, R.G. & Margolis, L.
      Preferential coreceptor utilization and cytopathicity by dual-tropic HIV-1 in human lymphoid tissue ex vivo.
      J. Clin. Invest., 104: R7-R11 (1999).
      


1115. Arranz, M.E., Díaz, J.A., Ingate, S.T., Witvrouw, M., Pannecouque, C., Balzarini, J., De Clercq, E. & Vega, S.
      Synthesis and anti-HIV activity of 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazines (TTDs): a new family of HIV-1-specific non-nucleoside reverse transcriptase inhibitors.
      Bioorg. Med. Chem., 7: 2811-2822 (1999).
      


1116. Velázquez, S., Tunón, V., Jimeno, M.L., Chamorro, C., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Potential multifunctional inhibitors of HIV-1 reverse transcriptase. Novel [AZT]-[TSAO-T] and [d4T]-[TSAO-T] heterodimers modified in the linker and in the dideoxynucleoside region.
      J. Med. Chem., 42: 5188-5196 (1999).
      


1117. Neyts, J., Leyssen, P. & De Clercq, E.
      Infections with flaviviridae.
      Verh. K. Acad. Geneesk. Belg., 61: 661-699 (1999).
      


1118. Van Gelder, J., Witvrouw, M., Pannecouque, C., Henson, G., Bridger, G., Naesens, L., De Clercq, E., Annaert, P., Shafiee, M., Van den Mooter, G., Kinget, R. & Augustijns, P.
      Evaluation of the potential of ion pair formation to improve the oral absorption of two potent antiviral compounds, AMD3100 and PMPA.
      Int. J. Pharm., 186: 127-136 (1999).
      


1119. Neyts, J. & De Clercq, E.
      Hydroxyurea potentiates the antiherpesvirus activities of purine and pyrimidine nucleoside and nucleotide phosphonate analogs.
      Antimicrob. Agents Chemother., 43: 2885-2892 (1999).
      


1120. Van Laethem, K., Van Vaerenbergh, K., Schmit, J.-C., Sprecher, S., Hermans, P., De Vroey, V., Schuurman, R., Harrer, T., Witvrouw, M., Van Wijngaerden, E., Stuyver, L., Van Ranst, M., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Phenotypic assays and sequencing are less sensitive than point mutation assays for detection of resistance in mixed HIV-1 genotypic populations.
      J. Acquir. Immun. Defic. Syndrom. Hum. Retrovirol., 22: 107-118 (1999).
      


1121. Balzarini, J., Naesens, L., Aquaro, S., Knispel, T., Perno, C.-F., De Clercq, E. & Meier, C.
      Intracellular metabolism of CycloSaligenyl 3’-azido-2’,3’-dideoxythymidine monophos-phate, a prodrug of 3’-azido-2’,3’-dideoxythymidine (zidovudine).
      Mol. Pharmacol., 56: 1354-1361 (1999).
      


1122. Naesens, L., Hatse, S., Segers, C., Verbeken, E., De Clercq, E., Waer, M. & Balzarini, J.
      9-(2-Phosphonylmethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine: a novel prodrug of 9-(2-phosphonylmethoxyethyl)guanine with improved antitumor efficacy and selectivity in choriocarcinoma-bearing rats.
      Oncol. Res., 11: 195-203 (1999).
      


1123. Wera, S., Degrève, B., Balzarini, J., De Clercq, E. Thevelein, J.M. & Neyts, J.
      Budding yeast as a screening tool for discovery of nucleoside analogs for use in HSV-1 TK suicide gene therapy.
      BioTechniques, 27: 772-777 (1999).
      


1124. Nieto, M.I., Blanco, J.M., Caamano, O., Fernández, F., García-Mera, X., López, C., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of carbocyclic nucleosides incorporating a modified cyclopentane ring. Part 3: Adenosine and uridine analogues.
      Nucleosides & Nucleotides, 18: 2253-2263 (1999).
      


1125. Figueira, M.J., Blanco, J.M., Caamano, O., Fernández, F., García-Mera, X., López, C., Andrei, G., Snoeck, R., Padalko, E., Neyts, J., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral and cytostatic activities of carbocyclic nucleosides incorporating a modified cyclobutane ring. I: Guanosine analogues.
      Arch. Pharm. Pharm. Med. Chem., 332: 348-352 (1999).
      


1126. Blanco, J.M., Caamano, O., Fernández, F., García-Mera, X., Hergueta, A.R., López, C., Rodríguez-Borges, J.E., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral and antineoplastic activities of some novel carbocyclic guanosine analogues with a cyclobutane ring.
      Chem. Pharm. Bull., 47: 1314-1317 (1999).
      


1127. Degrève, B., Esnouf, R., De Clercq, E. & Balzarini, J.
      Characterization of multiple nuclear localization signals in herpes simplex virus type 1 thymidine kinase.
      Biochem. Biophys. Res. Commun., 264: 338-342 (1999).
      


1128. Cabrera, C., Witvrouw, M., Gutiérrez, A., Clotet, B., Kuipers, M.E., Swart, P.J., Meijer, D.K.F., Desmyter, J., De Clercq, E. & Esté, J.A.
      Resistance of the human immunodeficiency virus to the inhibitory action of negatively charged albumins on virus binding to CD4.
      AIDS Res. Hum. Retrovir., 15: 1535-1543 (1999).
      


1129. McGuigan, C., Yarnold, C.J., Jones, G., Velázquez, S., Barucki, H., Brancale, A., Andrei, G., Snoeck, R., De Clercq, E. & Balzarini, J.
      Potent and selective inhibition of varicella-zoster virus (VZV) by nucleoside analogues with an unusual bicyclic base.
      J. Med. Chem., 42: 4479-4484 (1999).
      


1130. Neyts, J. & De Clercq, E.
      Potentiation of the anti-herpesvirus activity of guanosine analogues by the immunosuppressive agent mycophenolate mofetil (Pointer).
      Int. Antiviral News, 7: 134-136 (1999).
      


1131. Yi, Y., Isaacs, S.N., Williams, D.A., Frank, I., Schols, D., De Clercq, E., Kolson, D.L. & Collman, R.G.
      Role of CXCR4 in cell-cell fusion and infection of monocyte-derived macrophages by primary human immunodeficiency virus type 1 (HIV-1) strains: two distinct mechanisms of HIV-1 dual tropism.
      J. Virol., 73: 7117-7125 (1999).
      


1132. Siddiqui, A.Q., McGuigan, C., Ballatore, C., Zuccotto, F., Gilbert, I.H., De Clercq, E. & Balzarini, J.
      Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR.
      J. Med. Chem., 42: 4122-4128 (1999).
      


1133. Inguaggiato, G., Hughes, D., De Clercq, E., Balzarini, J. & Simons, C.
      Novel 6-azapyrimidine-2’-deoxy-4’-thionucleosides: synthesis, biological evaluation and conformational analysis.
      Antiviral Chem. Chemother., 10: 241-249 (1999).
      


1134. Saboulard, D., Naesens, L., Cahard, D., Salgado, A., Pathirana, R., Velazquez, S., McGuigan, C., De Clercq, E. & Balzarini, J.
      Characterization of the activation pathway of phosphoramidate triester prodrugs of stavudine and zidovudine.
      Mol. Pharmacol., 56: 693-704 (1999).
      


1135. Tanaka, H., Hayakawa, H., Haraguchi, K., Miyasaka, T., Walker, R.T., De Clercq, E., Baba, M., Stammers, D.K. & Stuart, D.I.
      HEPT: from an investigation of lithiation of nucleosides towards a rational design of non-nucleoside reverse transcriptase inhibitors of HIV-1.
      In: “Advances in Antiviral Drug Design”, vol. 3, E. De Clercq (ed.). JAI Press Inc., Greenwich, Connecticut, USA, pp. 93-144 (1999).
      


1136. Bridger, G.J., Skerlj, R.T., Padmanabhan, S., Martellucci, S.A., Henson, G.W., Struyf, S., Witvrouw, M., Schols, D. & De Clercq, E.
      Synthesis and structure-activity relationships of phenylenebis(methylene)-linked Bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.
      J. Med. Chem., 42: 3971-3981 (1999).
      


1137. Kuipers, M.E., Swart, P.J., Witvrouw, M., Esté, J.A., Reymen, D., De Clercq, E. & Meijer, D.K.F.
      Anti-HIV-1 activity of combinations and covalent conjugates of negatively charged human serum albumins (NCAs) and AZT.
      J. Drug Targeting, 6: 323-335 (1999).
      


1138. Siddiqui, A.Q., McGuigan, C., Ballatore, C., Wedgwood, O., De Clercq, E. & Balzarini, J.
      Simple mono-derivatisation of the aryl moiety of d4A and ddA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.
      Bioorg. Med. Chem. Lett., 9: 2555-2560 (1999).
      


1139. Van Gelder, J., Annaert, P., Naesens, L., De Clercq, E., Van den Mooter, G., Kinget, R. & Augustijns, P.
      Inhibition of intestinal metabolism of the antiviral ester prodrug bis(POC)-PMPA by nature-identical fruit extracts as a strategy to enhance its oral absorption: an in vitro study.
      Pharm. Res., 16: 1035-1040 (1999).
      


1140. Manfredini, S., Baraldi, P.G., Durini, E., Vertuani, S., Balzarini, J., De Clercq, E., Karlsson, A., Buzzoni, V. & Thelander, L.
      5’-Phosphoramidates and 5’-diphosphates of 2’-O-allyl--D-arabinofuranosyl-uracil,
      -cytosine, and -adenine: inhibition of ribonucleotide reductase.
      J. Med. Chem., 42: 3243-3250 (1999).
      


1141. Ying, C., Van Pelt, J., Yap, S.H., De Clercq, E. & Neyts, J.
      Use of digoxigenin-labelled probes for the quantitation of HBV-DNA in antiviral drug evaluation.
      J. Virol. Methods, 81: 155-158 (1999).
      


1142. Martínez, A., Esteban, A.I., Herrero, A., Ochoa, C., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Imidazothiadiazine dioxides: synthesis and antiviral activity.
      Bioorg. Med. Chem., 7: 1617-1623 (1999).
      


1143. Ruell, J.A., De Clercq, E., Pannecouque, C., Witvrouw, M., Stup, T.L., Turpin, J.A., Buckheit, R.W. Jr. & Cushman, M.
      Synthesis and anti-HIV activity of cosalane analogues with substituted benzoic acid rings attached to the pharmacophore through methylene and amide linkers.
      J. Org. Chem., 64: 5858-5866 (1999).
      


1144. Menten, P., Struyf, S., Schutyser, E., Wuyts, A., De Clercq, E., Schols, D., Proost, P. & Van Damme, J.
      The LD78 isoform of MIP-1 is the most potent CCR5 agonist and HIV-1-inhibiting chemokine.
      J. Clin. Invest., 104: R1-R5 (1999).
      


1145. Zhang, Y., Schols, D. & De Clercq, E.
      Selective activity of various antiviral compounds against HHV-7 infection.
      Antiviral Res., 43: 23-35 (1999).
      


1146. Chimirri, A., Grasso, S., Monforte, P., Rao, A., Zappalà, M., Monforte, A.M., Pannecouque, C., Witvrouw, M., Balzarini, J. & De Clercq, E.
      Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
      Antiviral Chem. Chemother., 10: 211-217 (1999).
      


1147. Egberink, H.F., De Clercq, E., Van Vliet, A.L.W., Balzarini, J., Bridger, G.J., Henson, G., Horzinek, M.C. & Schols, D.
      Bicyclams, selective antagonists of the human chemokine receptor CXCR4, strongly inhibit feline immunodeficiency virus replication.
      J. Virol., 73: 6346-6352 (1999).
      


1148. De Clercq, E.
      Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists.
      Eur. Cytokine Network, 10: 281-285 (1999).
      


1149. Witvrouw, M., Pannecouque, C., Van Laethem, K., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV.
      AIDS, 13: 1477-1483 (1999).
      


1150. Hatse, S., De Clercq, E. & Balzarini, J.
      Role of antimetabolites of purine and pyrimidine nucleotide metabolism in tumor cell differentiation.
      Biochem. Pharmacol., 58: 539-555 (1999).
      


1151. Velázquez, S., Tunón, V., Jimeno, M.L., Pérez-Pérez, M.J., San-Félix, A., Chamorro, C., Lobatón, E., Esteban-Gamboa, A., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 1029-1030 (1999).
      


1152. Manfredini, S., Baraldi, P.G., Durini, E., Balzarini, J., De Clercq, E., Karlsson, A., Buzzoni, V. & Thelander, L.
      Synthesis, cytostatic activity and inhibition of ribonucleotide reductase by 5’-phosphoramidates and 5’-diphosphates, of 2’-O-allyl-arabinofuranosyl nucleosides.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 1007-1008 (1999).
      


1153. Bazzanini, R., Manfredini, S., Durini, E., Gröschel, B., Cinatl, J., Balzarini, J., De Clercq, E., Imbach, J.-L., Périgaud, C. & Gosselin, G.
      Prodrugs of ara-CMP and ara-AMP with a S-acyl-2-thioethyl (SATE) biolabile phosphate protecting group: synthesis and biological evaluation.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 971-972 (1999).
      


1154. Ballatore, C., McGuigan, C., De Clercq, E. & Balzarini, J.
      An in situ pig liver esterase assay as a useful predictive tool for the likely in vitro antiviral activity of phosphoramidate pro-drugs.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 967-969 (1999).
      


1155. Meier, C., Knispel, T., Marquez, V.E., De Clercq, E. & Balzarini, J.
      CycloSal-2’-ara(ribo)-fluoro-2’,3’-dideoxyadenosine monophosphates – an effort to solve the structure-activity relationship of 2’-fluoro-ddA.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 907-912 (1999).
      


1156. De Clercq, E., Andrei, G., Balzarini, J., Hatse, S., Liekens, S., Naesens, L., Neyts, J. & Snoeck, R.
      Antitumor potential of acyclic nucleosides phosphonates.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 759-771 (1999).
      


1157. Santana, L., Teijeira, M., Uriarte, E., Terán, C., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of 1,2-disubstituted carbonucleosides of 6-substituted purine and 8-azapurine.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 733-734 (1999).
      


1158. Chamorro, C., Velázquez, S., Jimeno, M.L., Pérez-Pérez, M.J., Lobatón, E., Tunón, V., Esteban-Gamboa, A., Gago, F., De Clercq, E., Balzarini, J., Camarasa, M.J. & San-Félix, A.
      Unexpected results in the reaction of 5’-tosyl TSAO-m3T with amines.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 715-716 (1999).
      


1159. Lobatón, E., Velázquez, S., San-Félix, A., Chamorro, C., Tunón, V., Esteban-Gamboa, A., De Clercq, E., Balzarini, J., Camarasa, M.J. & Pérez-Pérez, M.J.
      Novel TSAO derivatives modified at positions 3” and 4” of the spiro moiety.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 675-676 (1999).
      


1160. Pierra, C., Gosselin, G., Sommadossi, J.-P., Faraj, A., De Clercq, E., Balzarini, J. & Imbach, J.-L.
      Stereospecific synthesis and antiviral activities of -L-2’,3’-dideoxy-5-chloropyrimidine nucleoside derivatives.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 643-644 (1999).
      


1161. Nieto, I., Figueira, M.J., Blanco, J.M., Caamano, O., Fernández, F., De Clercq, E. & Balzarini, J.
      Synthesis of novel carbocyclic nucleosides with a modified cyclopentane ring and evaluation of their antiviral activity.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 641-642 (1999).
      


1162. Fedorov, I., Kazmina, E., Jasko, M., Balzarini, J., De Clercq, E., Sommadossi, J.-P., Imbach, J.-L. & Gosselin, G.
      3’-(N-Hydroxyimino)-2’,3’-dideoxynucleosides and their derivatives: synthesis, broad spectrum antiviral properties and synthetical application for the preparation of other nucleoside analogues.
      Proceedings of the XIIIth International Round Table on Nucleosides, Nucleotides, and their Biological Applications, Part I, Montpellier, France September 6-10, 1998.
      Nucleosides & Nucleotides, 18: 633-634 (1999).
      


1163. Raic-Malic, S., Hergold-Brundic, A., Nagl, A., Grdisa, M., Pavelic, K., De Clercq, E. and Mintas, M.
      Novel pyrimidine and purine derivatives of L-ascorbic acid: synthesis and biological evaluation.
      J. Med. Chem., 42: 2673-2678 (1999).
      


1164. Liekens, S., Leali, D., Neyts, J., Esnouf, R., Rusnati, M., Dell’era, P., Maudgal, P.C., De Clercq, E. & Presta, M.
      Modulation of fibroblast growth factor-2 receptor binding, signaling, and mitogenic activity by heparin-mimicking polysulfonated compounds.
      Mol. Pharmacol., 56: 204-213 (1999).
      


1165. Hatse, S., Schols, D., De Clercq, E. & Balzarini, J.
      9-(2-Phosphonylmethoxyethyl)adenine induces tumor cell differentiation or cell death by blocking cell cycle progression through the S phase.
      Cell Growth Differ., 10: 435-446 (1999).
      


1166. Esté, J.A., Cabrera, C., Blanco, J., Gutierrez, A., Bridger, G., Henson, G., Clotet, B., Schols, D. & De Clercq, E.
      Shift of clinical human immunodeficiency virus type 1 isolates from X4 to R5 and prevention of emergence of the syncytium-inducing phenotype by blockade of CXCR4.
      J. Virol., 73: 5577-5585 (1999).
      


1167. Breistøl, K., Balzarini, J., Sandvold, M.L., Myhren, F., Martinsen, M., De Clercq, E. & Fodstad, Ø.
      Antitumor activity of P-4055 (elaidic acid-cytarabine) compared to cytarabine in metastatic and s.c. human tumor xenograft models.
      Cancer Res., 59: 2944-2949 (1999).
      


1168. Thormar, H., Bergsson, G., Gonnarsson, E., Georgsson, G., Witvrouw, M., Steingrímsson, O., De Clercq, E. & Kristmundsdóttir, T.
      Hydrogels containing monocaprin have potent microbicidal activities against sexually transmitted viruses and bacteria in vitro.
      Sex. Transm. Infect., 75: 181-185 (1999).
      


1169. Holý, A., Günter, J., Dvoráková, H., Masojidková, M., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Structure-antiviral activity relationship in the series of pyrimidine and purine N-[2-(2-phosphonomethoxy)ethyl] nucleotide analogues. 1. Derivatives substituted at the carbon atoms of the base
      J. Med. Chem., 42: 2064-2086 (1999).
      


1170. Hatse, S., Naesens, L., De Clercq, E. & Balzarini, J.
      N6-Cyclopropyl-PMEDAP: a novel derivative of 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) with distinct metabolic, antiproliferative, and differentiation-inducing properties.
      Biochem. Pharmacol., 58: 311-323 (1999).
      


1171. De Clercq, E
      Perspectives for the treatment of hepatitis B virus infections.
      Int. J. Antimicrob. Agents, 12: 81-95 (1999).
      


1172. Snoeck, R. & De Clercq, E.
      Treatment of herpes simplex virus infections.
      Infections in Medicine, 16: 249,250,256,257,261-265 (1999).
      


1173. Vandamme, A.-M., Van Laethem, K., Schmit, J.-C., Van Wijngaerden, E., Reynders, M., Debyser, Z., Witvrouw, M., Van Ranst, M., De Clercq, E. & Desmyter, J.
      Long-term stability of human immunodeficiency virus viral load and infectivity in whole blood.
      Eur. J. Clin. Invest., 29: 445-452 (1999).
      


1174. Simonart, T., Andrei, G., Parent, D., Van Vooren, J.-P., De Clercq, E. & Snoeck, R.
      In vitro sensitivity of Kaposi’s sarcoma cells to various chemotherapeutic agents including acyclic nucleoside phosphonates.
      Antiviral Chem. Chemother., 10: 129-134 (1999).
      


1175. Pluymers, W., Cherepanov, P., Schols, D., De Clercq, E. & Debyser, Z.
      Nuclear localization of human immunodeficiency virus type 1 integrase expressed as a fusion protein with green fluorescent protein.
      Virology, 258: 327-332(1999).
      


1176. Liekens, S., Verbeken, E. Vandeputte, M., De Clercq, E. & Neyts, J.
      A novel animal model for hemangiomas: inhibition of hemangioma development by the angiogenesis inhibitor TNP-470.
      Cancer Res., 59: 2376-2383 (1999).
      


1177. Smeijsters, L.J.J.W., Franssen, F.F.J., Naesens, L., de Vries, E., Holý, A., Balzarini, J., De Clercq, E. & Overdulve, J.P.
      Inhibition of the in vitro growth of Plasmodium falciparum by acyclic nucleoside phosphonates.
      Int. J. Antimicrob. Agents., 12: 53-61(1999).
      


1178. Cherepanov, P., Surratt, D., Toelen, J., Pluymers, W., Griffith, J., De Clercq, E. & Debyser, Z.
      Activity of recombinant HIV-1 integrase on mini-HIV DNA.
      Nucleic Acids Res., 27: 2202-2210 (1999).
      


1179. Cushman, M., Insaf, S., Paul, G., Ruell, J.A., De Clercq, E., Schols, D., Pannecouque, C., Witvrouw, M., Schaeffer, C.A., Turpin, J.A., Williamson, K. & Rice, W.G.
      Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency.
      J. Med. Chem., 42: 1767-1777 (1999).
      


1180. Witvrouw, M., Pannecouque, C., De Clercq, E., Fernández-Alvarez, E. & Marco, J.L.
      Inhibition of human immunodeficiency virus type 1 (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.
      Arch. Pharm. Pharm. Med. Chem., 332: 163-166 (1999).
      


1181. Meier, C., Knispel, T., Marquez, V.E., De Clercq, E. & Balzarini, J.
      cycloSal-Pronucleotides of 2’-fluoro-ara- and 2’-fluoro-ribo-2’,3’-dideoxyadenosine as a strategy to bypass a metabolic blockade.
      J. Med. Chem., 42: 1615-1624 (1999).
      


1182. Meier, C., Knispel, T., De Clercq, E. & Balzarini, J.
      cycloSal-Pronucleotides of 2’,3’-dideoxyadenosine and 2’,3’-dideoxy-2’,3’-didehydroadenosine: synthesis and antiviral evaluation of a highly efficient nucleotide delivery system.
      J. Med. Chem., 42: 1604-1614 (1999).
      


1183. Molina, S., Cobo, J., Sánchez, A., Nogueras, M. & De Clercq, E.
      Synthesis and antiviral evaluation of several 6-(methylenecarbomethoxy)pteridin-4,7(3H,8H)-diones.
      J. Heterocyclic Chem., 36: 435-440 (1999).
      


1184. De Clercq, E.
      Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
      Proceedings of the “XIV Convegno Nazionale Divisione Chimica Farmaceutica – Società Chimica Italiana”, Salsomaggiore Terme, Parma, Italy, September 21-25, 1998.
      Il Farmaco, 54: 26-45 (1999).
      


1185. Lin, Z., Neamati, N., Zhao, H., Kiryu, Y., Turpin, J.A., Aberham, C., Strebel, K., Kohn, K., Witvrouw, M., Pannecouque, C., Debyser, Z., De Clercq, E., Rice, W.G., Pommier, Y. & Burke, T.R. Jr.
      Chicoric acid analogues as HIV-1 integrase inhibitors.
      J. Med. Chem., 42: 1401-1414 (1999).
      


1186. Dimmock, J.R., Kandepu, N.M., Nazarali, A.J., Kowalchuk, T.P., Motaganahalli, N., Quail, J.W., Mykytiuk, P.A., Audette, G.F., Prasad, L., Perjési, P., Allen, T.M., Santos, C.L., Szydlowski, J., De Clercq, E. & Balzarini, J.
      Conformational and quantitative structure – activity relationship study of cytotoxic 2-arylidenebenzocycloalkanones.
      J. Med. Chem., 42: 1358-1366 (1999).
      


1187. Struyf, S., Proost, P., Schols, D., De Clercq, E., Opdenakker, G., Lenaerts, J.-P., Detheux, M., Parmentier, M., De Meester, I., Scharpé, S. & Van Damme, J.
      CD26/dipeptidyl-peptidase IV down-regulates the eosinophil chemotactic potency, but not the anti-HIV activity of human eotaxin by affecting its interaction with CC chemokine receptor 3.
      J. Immunol., 162: 4903-4909 (1999).
      


1188. De Clercq, E.
      63. Antivirale Geneesmiddelen.
      In: “Algemene Farmacotherapie”, 7de druk. H. Wesseling, C. Neef & P.A. de Graeff (eds.). Bohn Stafleu Van Loghum, Houten, The Netherlands, pp. 869-881 (1999).
      


1189. Martinez, A., Esteban, A.I., Castro, A., Gil, C., Conde, S., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Novel potential agents for human cytomegalovirus infection: synthesis and antiviral activity evaluation of benzothiadiazine dioxide acyclonucleosides.
      J. Med. Chem., 42: 1145-1150 (1999).
      


1190. Niyonzima, G., Laekeman, G., Witvrouw, M., Van Poel, B., Pieters, L., Paper, D., De Clercq, E., Franz, G. & Vlietinck, A.J.
      Hypoglycemic, anticomplement and anti-HIV activities of Spathodea campanulata stem bark.
      Phytomedicine, 6: 45-49 (1999).
      


1191. Van Derpoorten, K., Ucar, H., Andrei, G., Snoeck, R., Balzarini, J., De Clercq, E. & Poupaert, J.
      Synthesis and antiviral activity of 6-benzoyl-benzoxazolin-2-one and 6-benzoyl-benzothiazolin-2-one derivatives.
      Antiviral Chem. Chemother., 10: 87-97 (1999).
      


1192. Neyts, J. & De Clercq, E.
      The immunosuppressive agent mycophenolate mofetil markedly potentiates the activity of lobucavir [1R(1,2,3)]-9-[2,3-bis(hydroxymethyl)cyclobutyl]guanine against different herpes viruses.
      Transplantation, 67: 760-764 (1999).
      


1193. De Clercq, E., Plattner, J.J. & Chu, D.T.
      Editorial. An introduction to current opinion in anti-infective investigational drugs
      Curr. Opin. Anti-infect. Invest. Drugs, 1: 1-3 (1999).
      


1194. Hatse, S., De Clercq, E. & Balzarini, J.
      Impact of 9-(2-phosphonylmethoxyethyl)adenine on (deoxy)ribonucleotide metabolism and nucleic acid synthesis in tumor cells.
      FEBS Lett., 445: 92-97 (1999).
      


1195. Daelemans, D., Vandamme, A.-M. & De Clercq, E.
      Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy.
      Antiviral Chem. Chemother., 10: 1-14 (1999).
      


1196. Degrève, B., De Clercq, E. & Balzarini, J.
      Bystander effect of purine nucleoside analogues in HSV-1tk suicide gene therapy is superior to that of pyrimidine nucleoside analogues.
      Gene Ther., 6: 162-170 (1999).
      


1197. Ghosh, A., Miller, M.J., De Clercq, E. & Balzarini, J.
      Synthesis and biological evaluation of a carbocyclic azanoraristeromycin siderophore conjugate.
      Nucleosides & Nucleotides, 18: 217-225 (1999).
      


1198. McGuigan, C., Siddiqui, A.Q., Ballatore, C., De Clercq, E. & Balzarini, J.
      The presence of substituents on the aryl moiety of the aryl phosphoramidate derivative of d4T enhances anti-HIV efficacy in cell culture: a structure-activity relationship.
      J. Med. Chem., 42: 393-399 (1999).
      


1199. Esté, J.A., Cabrera, C., De Clercq, E., Struyf, S., Van Damme, J., Bridger, G., Skerlj, R.T., Abrams, M.J., Henson, G., Gutierrez, A., Clotet, B. & Schols, D.
      Activity of different bicyclam derivatives against human immunodeficiency virus depends on their interaction with the CXCR4 chemokine receptor.
      Mol. Pharmacol., 55: 67-73 (1999).
      



118 publications in the year 1998



1200. Hossain, N., Van Halbeek, H., De Clercq, E. & Herdewijn, P.
      Synthesis of 3’-C-branched 1’,5’-anhydromannitol nucleosides as new antiherpes agents.
      Tetrahedron, 54: 2209-2226 (1998).
      


1201. De Clercq, E.
      New perspectives for the treatment of HIV infections.
      Proceedings of the 19° Congresso Nazionale della Societa’ Italiana di Chemioterapia, Giardini Naxos, Italy, June 11-14, 1997.
      Il Giornale Italiano di Chemioterapia, 45: 9-16 (1998).
      


1202. Simonart, T., Noel, J.-C., De Dobbeleer, G., Parent, D., Van Vooren, J.-P., De Clercq, E. & Snoeck, R.
      Treatment of classical Kaposi’s sarcoma with intralesional injections of cidofovir: report of a case.
      J. Med. Virol., 55: 215-218 (1998).
      


1203. Andrei, G., Snoeck, R., Piette, J., Delvenne, P. & De Clercq, E.
      Inhibitory effects of cidofovir (HPMPC) on the growth of the human cervical carcinoma (SiHa) xenografts in athymic-nude mice.
      Oncol. Res., 10: 533-539 (1998).
      


1204. Andrei, G., Snoeck, R., Piette, J., Delvenne, P. & De Clercq, E.
      Antiproliferative effects of acyclic nucleoside phosphonates on human papillomavirus (HPV)-harboring cell lines compared with HPV-negative cell lines.
      Oncol. Res., 10: 523-531 (1998).
      


1205. Tusek-Bozic, L., Furlani, A., Scarcia, V., De Clercq, E. & Balzarini, J.
      Spectroscopic and biological properties of palladium(II) complexes of ethyl-2-quinolylmethylphosphonate.
      J. Inorg. Biochem., 72: 201-210 (1998).
      


1206. Vamecq, J., Vanderpoorten, K., Poupaert, J.H., Balzarini, J., De Clercq, E. & Stables, J.P.
      Anticonvulsant phenytoinergic pharmacophores and anti-HIV activity – Preliminary evidence for the dual requirement of the 4-aminophthalimide platform and the N-(1-adamantyl) substitution for antiviral properties.
      Life Sci., 63: PL267-PL274 (1998).
      


1207. McGuigan, C., Cahard, D., Ballatore, C., Siddiqui, A., De Clercq, E. & Balzarini, J.
      Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs – despite efficient esterase-mediated hydrolysis.
      Bioorg. Med. Chem. Lett., 8: 2949-2954 (1998).
      


1208. Banker, A.S., Bergeron-Lynn, G., Keefe, K.S., De Clercq, E., Taskintuna, I. & Freeman, W.R.
      Effects of topical and subconjunctival cidofovir (HPMPC) in an animal model.
      Curr. Eye Res., 17: 560-566 (1998).
      


1209. Santana, L., Teijeira, M., Uriarte, E., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of 1,2-disubstituted carbonucleosides of 2-amino-6-substituted purine and 8-azapurine.
      Bioorg. Med. Chem. Lett., 8: 1349-1352 (1998).
      


1210. Balzarini, J., Pelemans, H., De Clercq, E., Dunkler, A. & Kleim, J.-P.
      Combination of the multidrug resistance mutation Q151M/L and the AZT resistance mutation T215Y/F in the same HIV-1 reverse transcriptase is compatible with enzymatic activity.
      Proceedings of the 12th World AIDS Conference, Geneva, June 28-July 3, 1998. Monduzzi Editore, Int. Proc. Div., Bologna, Italy, pp. 319-323 (1998).
      


1211. Balzarini, J., Naesens, L., Verbeken, E., Laga, M., Van Damme, L., Verstraeten, M., Van Mellaert, L., Anné, J. & De Clercq, E.
      The thiocarboxanilide UC-781 is a potential virucidal drug.
      Proceedings of the 12th World AIDS Conference, Geneva, June 28-July 3, 1998. Monduzzi Editore, Int. Proc. Div., Bologna, Italy, pp. 243-247 (1998).
      


1212. Annaert, P., Van Gelder, J., Naesens, L., De Clercq, E., Van den Mooter, G., Kinget, R. & Augustijns, P.
      Carrier mechanisms involved in the transepithelial transport of bis(POM)-PMEA and its metabolites across Caco-2 monolayers.
      Pharm. Res., 15: 1168-1173 (1998).
      


1213. Meier, C., De Clercq, E. & Balzarini, J.
      Nucleotide delivery from cycloSaligenyl-3’-azido-3’-deoxythymidine monophosphates (cycloSal-AZTMP).
      Eur. J. Org. Chem., 1998: 837-846 (1998).
      


1214. Afouna, M.I., Mehta, S.C., Ghanem, A.-H., Higuchi, W.I., Kern, E.R., De Clercq, E. & El-Shattaway, H.H.
      Assessment of correlation between skin target site free drug concentration and the in vivo topical antiviral efficacy in hairless mice for (E)-5-(2-bromovinyl)-2’-deoxyuridine and acyclovir formulations.
      J. Pharm. Sci., 87: 917-921 (1998).
      


1215. Papakonstantinou-Garoufalia, S.S., Tani, E., Todoulou, O., Papadaki-Valiraki, A., Filippatos, E., De Clercq, E. & Kourounakis, P.N.
      Synthesis and pharmacochemical investigation of some novel 1,2,4-4H-triazoles with potential antiviral activity.
      J. Pharm. Pharmacol., 50: 117-124 (1998).
      


1216. De Clercq, E.
      Novel approaches towards anti-HIV chemotherapy.
      Proceedings of the 11th Noordwijkerhout-Camerino Symposium on Trends in Drug Research, The Netherlands, 11-15 May 1997.
      In: “Trends in Drug Research II”, Proceedings of the 11th Noordwijkerhout-Camerino Symposium, 11-15 May 1997, Noordwijkerhout, The Netherlands, H. van der Goot (ed.), Pharmacochemistry Library, vol. 29, pp. 91-104, Elsevier Science B.V., Amsterdam, (1998).
      


1217. De Clercq, E.
      Antiviral agents that are active against CMV: potential of cidofovir for the treatment of CMV and other virus infections.
      Proceedings of the First International Consensus Round Table Meeting on CMV-Related Immunopathology, Frankfurt, Germany, 28-30 August 1997.
      In: “CMV-Related Immunopathology”, Monographs in Virology, vol. 25. M. Scholz, H.F. Rabenau, H.W. Doerr & J. Cinatl. Jr. (eds.), Karger Verlag, Basel, pp. 193-214 (1998).
      


1218. Vandamme, A.-M., Van Laethem, K., Van Vaerenbergh, K. & De Clercq, E.
      Anti-HIV virus combination therapy and resistance management.
      Int. Antiviral News, 6: 182-187 (1998).
      


1219. Snoeck, R., Andrei, G. & De Clercq, E.
      Specific therapies for human papilloma virus infections.
      Curr. Opin. Infect. Dis., 11: 733-737 (1998).
      


1220. Schmit, J.-C., Ruiz, L., Stuyver, L., Van Laethem, K., Vanderlinden, I., Puig, T., Rossau, R., Desmyter, J., De Clercq, E., Clotet, B. & Vandamme, A.-M.
      Comparison of the LiPA HIV-1 RT test, selective PCR and direct solid phase sequencing for the detection of HIV-1 drug resistance mutations.
      J. Virol. Methods, 73: 77-82 (1998).
      


1221. Manfredini, S., Simoni, D., Caminiti, G., Vertuani, S., Invidiata, F., Moscato, B., Hatse, S., De Clercq, E. & Balzarini, J.
      Retinoids as potential chemotherapeutic agents. Synthesis, cytostatic and differentiating activities of new heterocyclic analogues of retinoic acid.
      Med. Chem. Res., 8: 291-304 (1998).
      


1222. Pelemans, H., Esnouf, R., Jonckheere, H., De Clercq, E. & Balzarini, J.
      Mutational analysis of Tyr-318 within the non-nucleoside reverse transcriptase inhibitor binding pocket of human immunodeficiency virus type 1 reverse transcriptase.
      J. Biol. Chem., 273: 34234-34239 (1998).
      


1223. Neyts, J., Andrei, G. & De Clercq, E.
      The antiherpesvirus activity of H2G [(R)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine] is markedly enhanced by the novel immunosuppressive agent mycophenolate mofetil.
      Antimicrob. Agents Chemother., 42: 3285-3289 (1998).
      


1224. Van hemel, J., Esmans, E.L., Joos, P.E., De Groot, A., Dommisse, R.A., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of phosphonate derivatives of some acyclic pyridine-C-nucleosides.
      Nucleosides & Nucleotides, 17: 2429-2443 (1998).
      


1225. Al-Masoudi, N.A., Al-Soud, Y.A., Ehrmann, M. & De Clercq, E.
      Quinolone nucleosides: 6,7-dihalo-N-- and -glycoysl-1,4-dihydro-4-oxo-quinoline-3-carboxylic acids and derivatives. Synthesis, antimicrobial and antiviral activity.
      Nucleosides & Nucleotides, 17: 2255-2266 (1998).
      


1226. Gueiffier, A., Mavel, S., Lhassani, M., Elhakmaoui, A., Snoeck, R., Andrei, G., Chavignon, O., Teulade, J.-C., Witvrouw, M., Balzarini, J., De Clercq, E. & Chapat, J.-P.
      Synthesis of imidazo[1,2-a]pyridines as antiviral agents.
      J. Med. Chem., 41: 5108-5112 (1998).
      


1227. Leydet, A., Moullet, C., Roque, J.P., Witvrouw, M., Pannecouque, C., Andrei, G., Snoeck, R., Neyts, J., Schols, D. & De Clercq, E.
      Polyanion inhibitors of HIV and other viruses. 7. Polyanionic compounds and polyzwitterionic compounds derived from cyclodextrins as inhibitors of HIV transmission.
      J. Med. Chem., 41: 4927-4932 (1998).
      


1228. Velázquez, S., Alvarez, R., Pérez, C., Gago, F., De Clercq, E., Balzarini, J. & Camarasa, M.-J.
      Regiospecific synthesis and anti-human immunodeficiency virus activity of novel 5-substituted N-alkylcarbamoyl and N,N-dialkyl carbamoyl 1,2,3-triazole-TSAO analogues.
      Antiviral Chem. Chemother., 9: 481-489 (1998).
      


1229. McGuigan, C., Sutton, P.W., Cahard, D., Turner, K., O’Leary, G., Wang, Y., De Clercq, E. & Balzarini, J.
      Synthesis, anti-human immunodeficiency virus activity and esterase lability of some novel carboxylic ester-modified phosphoramidate derivatives of stavudine (d4T).
      Antiviral Chem. Chemother., 9: 473-479 (1998).
      


1230. Hatse, S., De Clercq, E. & Balzarini, J.
      Enhanced 9-(2-phosphonylmethoxyethyl)adenine secretion by a specific, indomethacin-sensitive efflux pump in a mutant 9-(2-phosphonylmethoxyethyl)adenine-resistant human erythroleukemia K562 cell line.
      Mol. Pharmacol., 54: 907-917 (1998).
      


1231. Thormar, H., Georgsson, G., Pálsson, P.A., Gunnarsson, E., Torsteinsdóttir, S., Balzarini, J., Naesens, L. & De Clercq, E.
      Visna in sheep as a model for chemotherapy of lentiviral central nervous system infections.
      Proceedings of the Nordic Veterinary Conference, Reykjavik, Iceland, July 1996.
      Clin. Microbiol. Infect., 4: 618-621 (1998).
      


1232. Degrève, B., Johansson, M., De Clercq, E., Karlsson, A. & Balzarini, J.
      Differential intracellular compartmentalization of herpetic thymidine kinases (TKs) in TK gene-transfected tumor cells: molecular characterization of the nuclear localization signal of herpes simplex virus type 1 TK.
      J. Virol., 72: 9535-9543 (1998).
      


1233. Neyts, J. & De Clercq, E.
      Mycophenolate mofetil strongly potentiates the anti-herpesvirus activity of ayclovir.
      Antiviral Res., 40: 53-56 (1998).
      


1234. Kristmundsdóttir, T., Thormar, H., Witvrouw, M. & De Clercq, E.
      Evaluation of virucidal activity of hydrogels containing monoglyceride.
      Proceedings of the Symposium on “Natural Origin Substances in Drug Formulation”, Beijing, China, 4-6 November 1998, pp. 109-110 (1998).
      


1235. Balzarini, J., Esteban-Gamboa, A., Esnouf, R., Liekens, S., Neyts, J., De Clercq, E., Camarasa, M.-J. & Pérez-Pérez, M.J.
      7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
      FEBS Lett., 438: 91-95 (1998).
      


1236. Velázquez, S., Chamorro, C., Pérez-Pérez, M.-J., Alvarez, R., Jimeno, M.-L., Martín-Domenech, A., Pérez, C., Gago, F., De Clercq, E., Balzarini, J., San-Félix, A. & Camarasa, M.-J.
      Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase.
      J. Med. Chem., 41: 4636-4647 (1998).
      


1237. Proost, P., Struyf, S., Wuyts, A., Menten, P., De Meester, I., Lambeir, A.-M., Scharpé, S., Schols, D., De Clercq, E. & Van Damme, J.
      Isolation and identification of naturally modified C-C chemokines MCP-1, MCP-2 and RANTES: effects of posttranslational modifications on receptor usage, chemotactic and anti-HIV-1 activity.
      Proceedings of the Vth International Workshop on Cytokines, Florence, Italy, 16-18 March 1998.
      Eur. Cytokine Netw., 9, suppl. 3: 73-75 (1998).
      


1238. Schols, D., Proost, P., Struyf, S., Wuyts, A., De Meester, I., Scharpé, S., Van Damme, J. & De Clercq, E.
      CD26-processed RANTES(3-68), but not intact RANTES, has potent anti-HIV-1 activity.
      Antiviral Res., 39: 175-187 (1998).
      


1239. Esté, J. & De Clercq, E.
      Ajoene [(e,z)-4,5,9-trithiadodeca-1,6,11-triene 9 oxide] does not exhibit antiviral activity at subtoxic concentrations.
      Biomed. & Pharmacother., 52: 236-238 (1998).
      


1240. Ostrowski, T., Wroblowski, B., Busson, R., Rozenski, J., De Clercq, E., Bennett, M.S., Champness, J.N., Summers, W.C., Sanderson, M.R. & Herdewijn, P.
      5-Substituted pyrimidines with a 1,5-anhydro-2,3-dideoxy-D-arabino-hexitol moiety at N-1: synthesis, antiviral activity, conformational analysis, and interaction with viral thymidine kinase.
      J. Med. Chem., 41: 4343-4353 (1998).
      


1241. Balzarini, J. & De Clercq, E.
      Biochemical pharmacology. A. Nucleoside and non-nucleoside reverse transcriptase inhibitors active against HIV.
      In: “Textbook of AIDS Medicine”, 2nd Ed., T.C. Merigan, J.G. Bartlett & D. Bolognesi (eds.). Williams & Wilkins, Baltimore, Maryland, USA, pp. 815-847 (1998).
      


1242. Schmit, J.-C., Van Laethem, K., Ruiz, L., Hermans, P., Sprecher, S., Sönnerborg, A., Leal, M., Harrer, T., Clotet, B., Arendt, V., Lissen, E., Witvrouw, M., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Multiple dideoxynucleoside analogue-resistant (MddNR) HIV-1 strains isolated from patients from different European countries.
      AIDS, 12: 2005-2015 (1998).
      


1243. Pandeya, S.N., Sriram, D., De Clercq, E., Pannecouque, C. & Witvrouw, M.
      Anti-HIV activity of some Mannich bases of isatin derivatives.
      Indian J. Pharm. Sci., 60: 207-212 (1998).
      


1244. Arranz, E., Díaz, J.A., Ingate, S.T., Witvrouw, M., Pannecouque, C., Balzarini, J., De Clercq, E. & Vega, S.
      Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
      J. Med. Chem., 41: 4109-4117 (1998).
      


1245. Dimmock, J.R., Vashishtha, S.C., Quail, J.W., Pugazhenthi, U., Zimpel, Z., Sudom, A.M., Allen, T.M., Kao, G.Y., Balzarini, J. & De Clercq, E.
      4-(-Arylvinyl)-3-(-arylvinylketo)-1-ethyl-4-piperidinols and related compounds: a novel class of cytotoxic and anticancer cells.
      J. Med. Chem., 41: 4012-4020 (1998).
      


1246. Chimirri, A., Grasso, S., Monforte, A.M., Monforte, P., Rao, A., Zappalà, M., Bruno, G., Nicolò, F., Pannecouque, C., Witvrouw, M. & De Clercq, E.
      Synthesis, structure and in vitro anti-human immunodeficiency virus activity of novel 3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles.
      Antiviral Chem. Chemother., 9: 431-438 (1998).
      


1247. Chamorro, C., Camarasa, M.-J., Pérez-Pérez, M.-J., De Clercq, E., Balzarini, J. & San Félix, A.
      An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
      Antiviral Chem. Chemother., 9: 413-423 (1998).
      


1248. Witvrouw, M., Daelemans, D., Pannecouque, C., Neyts, J., Andrei, G., Snoeck, R., Vandamme, A.-M., Balzarini, J., Desmyter, J., Baba, M. & De Clercq, E.
      Broad-spectrum antiviral activity and mechanism of antiviral action of the fluoroquinolone derivative K-12.
      Antiviral Chem. Chemother., 9: 403-411 (1998).
      


1249. Robins, M.J., Wnuk, S.F., Yang, X., Yuan, C.-S., Borchardt, R.T., Balzarini, J. & De Clercq, E.
      Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5’,5’,6’,6’-tetradehydro-6’-deoxy-6’-halohomoadenosine analogues (4’-haloacetylene analogues derived from adenosine).
      J. Med. Chem., 41: 3857-3864 (1998).
      


1250. Balzarini, J., Naesens, L. & De Clercq, E.
      New antivirals – mechanism of action and resistance development.
      Curr. Opin. Microbiol., 1: 535-546 (1998).
      


1251. Hatse, S., Naesens, L., De Clercq, E. & Balzarini, J.
      Potent differentiation-inducing properties of the antiretroviral agent 9-(2-phosphonyl-methoxyethyl)adenine (PMEA) in the rat choriocarcinoma (RCHO) tumor cell model.
      Biochem. Pharmacol., 56: 851-859 (1998).
      


1252. Simmons, G., Reeves, J.D., McKnight, A., Dejucq, N., Hibbitts, S., Power, C.A., Aarons, E., Schols, D., De Clercq, E., Proudfoot, A.E.I., Weiss, R.A. & Clapham, P.R.
      CXCR4 as a functional coreceptor for human immunodeficiency virus type 1 infection of primary macrophages.
      J. Virol., 72: 8453-8457 (1998).
      


1253. Struyf, S., Proost, P., Sozzani, S., Mantovani, A., Wuyts, A., De Clercq, E., Schols, D. & Van Damme, J.
      Enhanced anti-HIV-1 activity and altered chemotactic potency of NH2-terminally processed macrophage-derived chemokine imply an additional MDC receptor. (Cutting Edge).
      J. Immunol., 161: 2672-2675 (1998).
      


1254. Labrosse, B., Brelot, A., Heveker, N., Sol, N., Schols, D., De Clercq, E. & Alizon, M.
      Determinants for sensitivity of human immunodeficiency virus coreceptor CXCR4 to the bicyclam AMD3100.
      J. Virol., 72: 6381-6388 (1998).
      


1255. Champness, J.N., Bennett, M.S., Wien, F., Visse, R., Summers, W.C., Herdewijn, P., De Clercq, E., Ostrowski, T., Jarvest, R.L. & Sanderson, M.R.
      Exploration of the active site of herpes simplex virus type-1 thymidine kinase by X-ray crystallography of complexes with aciclovir and other ligands.
      Proteins: Struct. Funct. & Genetics, 32: 350-361 (1998).
      


1256. Schols, D. & De Clercq, E.
      The simian immunodeficiency virus mnd(GB-1) strain uses CXCR4, not CCR5, as coreceptor for entry in human cells.
      J. Gen. Virol., 79: 2203-2205 (1998).
      


1257. De Clercq, E.
      The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
      Antiviral Res., 38: 153-179 (1998).
      


1258. Proost, P., Struyf, S., Schols, D., Durinx, C., Wuyts, A., Lenaerts, J.-P., De Clercq, E., De Meester, I. & Van Damme, J.
      Processing by CD26/dipeptidyl-peptidase IV reduces the chemotactic and anti-HIV-1 activity of stromal-cell-derived factor-1.
      FEBS Lett., 432: 73-76 (1998).
      


1259. Seley, K.L., Schneller, S.W., De Clercq, E., Rattendi, D., Lane, S., Bacchi, C.J. & Korba, B.
      The importance of the 4’-hydroxyl hydrogen for the antitrypanosomal and antiviral properties of (+)-5’-noraristeromycin and two 7-deaza analogues.
      Bioorg. Med. Chem., 6: 797-801 (1998).
      


1260. Suruga, Y., Makino, M., Okada, Y., Tanaka, H., De Clercq, E. & Baba, M.
      Prevention of murine AIDS development by (R)-9-(2-phosphonylmethoxypro-pyl)adenine.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 18: 316-322 (1998).
      


1261. Wnuk, S.F., Mao, Y., Yuan, C.-S., Borchardt, R.T., Andrei, G., Balzarini, J., De Clercq, E. & Robins, M.J.
      Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its “hydrolytic activity”. Synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine.
      J. Med. Chem., 41: 3078-3083 (1998).
      


1262. Schmit, J.-C., Martinez-Picado, J., Ruiz, L., Tural, C., Van Laethem, K., Cabrera, C., Ibanez, A., Puig, T., Witvrouw, M., Desmyter, J., De Clercq, E., Clotet, B. & Vandamme, A.-M.
      Evolution of HIV drug resistance in zidovudine/zalcitabine and zidovudine/didanosine-experienced patients receiving lamivudine-containing combination therapy.
      Antiviral Therapy, 3: 81-88 (1998).
      


1263. Van Laethem, K., Beuselinck, K., Van Dooren, S., De Clercq, E., Desmyter, J. & Vandamme, A.-M.
      Diagnosis of human immunodeficiency virus infection by a polymerase chain reaction assay evaluated in patients harbouring strains of diverse geographical origin.
      J. Virol. Methods, 70: 153-166 (1998).
      


1264. Naesens, L., Cahard, D., Salgado, A., Bidois, L., De Clercq, E., McGuigan, C. & Balzarini, J.
      Metabolism and anti-HIV activity of phosphoramidate derivatives of D4T-MP with variations in the amino acid moiety.
      Proceedings of the 9th International/6th European Joint Symposium on Purine & Pyrimidine Metabolism in Man, Gmunden, Austria, 1-7 June 1997.
      In: “Purine and Pyrimidine Metabolism in Man IX”, Griesmacher et al., Plenum Press, New York, pp. 753-757 (1998).
      


1265. Balzarini, J., Stet, L., Matsuda, A., Wiebe, L., Knauss, E. & De Clercq, E.
      Metabolism of EICAR (5-ethynyl-1--D-ribofuranosylimidazole-4-carboxamide), a potent inhibitor of inosinate dehydrogenase.
      Proceedings of the 9th International/6th European Joint Symposium on Purine & Pyrimidine Metabolism in Man, Gmunden, Austria, 1-7 June 1997.
      In: “Purine and Pyrimidine Metabolism in Man IX”, Griesmacher et al., Plenum Press, New York, pp. 723-728 (1998).
      


1266. Hatse, S., Naesens, L., Degrève, B., Vandeputte, M., Waer, M., De Clercq, E. & Balzarini, J.
      In vitro and in vivo inhibitory activity of the differentiation-inducing agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against rat choriocarcinoma.
      Proceedings of the 9th International/6th European Joint Symposium on Purine & Pyrimidine Metabolism in Man, Gmunden, Austria, 1-7 June 1997.
      In: “Purine and Pyrimidine Metabolism in Man IX”, Griesmacher et al., Plenum Press, New York, pp. 605-609 (1998).
      


1267. De Clercq, E.
      Recent developments in the chemotherapy of HIV infections.
      Proceedings of the AIMECS 97: International Medicinal Chemistry Symposium, Seoul, Korea, 27 July - 1 August 1997.
      Pure & Appl. Chem., 70: 567-577 (1998).
      


1268. Naesens, L., Bischofberger, N., Augustijns, P., Annaert, P., Van den Mooter, G., Arimilli, M.N., Kim, C.U. & De Clercq, E.
      Antiretroviral efficacy and pharmacokinetics of oral bis(isopropyloxy-carbonyloxy-methyl)-9-(2-phosphonylmethoxypropyl)adenine in mice.
      Antimicrob. Agents Chemother., 42: 1568-1573 (1998).
      


1269. De Clercq, E.
      New perspectives for the treatment of HIV infections.
      Proceedings of the IVth Congress of the Mediterranean Society of Infectious and Parasitic Diseases and the 1st Congress of the Arab Society of Chemotherapy, Microbiology and Infectious Diseases, Cairo, Egypt, 17-21 October 1997.
      Mediterranean Journal of Infectious and Parasitic Diseases, 13: 7-20 (1998).
      


1270. Liekens, S., Andrei, G., Vandeputte, M., De Clercq, E. & Neyts, J.
      Potent inhibition of hemangioma formation in rats by the acyclic nucleoside phosphonate analogue cidofovir
      Cancer Res., 58: 2562-2567 (1998).
      


1271. Balzarini, J., Naesens, L., Verbeken, E., Laga, M., Van Damme, L., Parniak, M., Van Mellaert, L., Anné, J. & De Clercq, E.
      Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent.
      AIDS, 12: 1129-1138 (1998).
      


1272. Pelemans, H., Esnouf, R.M., Parniak, M.A., Vandamme, A.-M., De Clercq, E. & Balzarini, J.
      A proline-to-histidine substitution at position 225 of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) sensitizes HIV-1 RT to BHAP U-90152.
      J. Gen Virol., 79: 1347-1352 (1998).
      


1273. Banker, A.S., De Clercq, E., Taskintuna, I., Keefe, K.S., Bergeron-Lynn, G. & Freeman, W.R.
      Influence of intravitreal injections of HPMPC and related nucleoside analogues on intraocular pressure in guinea pig eyes.
      Invest. Ophthalmol. Vis. Sci., 39: 1233-1242 (1998).
      


1274. Nieto, M.I., Blanco, J.M., Caamano, O., Fernández, F., García-Mera, X., Balzarini, J., Padalko, E., Neyts, J. & De Clercq, E.
      Synthesis, antiviral and cytostatic activities of carbocyclic nucleosides incorporating a modified cyclopentane ring. Part 2: Adenosine and uridine analogues.
      Nucleosides & Nucleotides, 17: 1255-1266 (1998).
      


1275. Borges, J.E.R., Fernández, F., Garciá, X., Hergueta, A.R., López, C., Andrei, G., Snoeck, R., Witvrouw, M., Balzarini, J. & De Clercq, E.
      Novel carbocyclic nucleosides containing a cyclobutyl ring: guanosine and adenosine analogues.
      Nucleosides & Nucleotides, 17: 1237-1253 (1998).
      


1276. De Clercq, E.
      Towards an effective chemotherapy of virus infections: Therapeutic potential of cidofovir [(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, HPMPC for the treatment of DNA virus infections.
      Collect. Czech. Chem. Commun., 63: 480-506 (1998).
      


1277. De Clercq, E.
      New perspectives for the treatment of HIV infections.
      Collect. Czech. Chem. Commun., 63: 449-479 (1998).
      


1278. De Clercq, E.
      Nieuwe perspectieven voor de behandeling van HIV-infecties.
      Tijdschr. Geneesk., 54: 773-782 (1998).
      


1279. Meerbach, A., Neyts, J., Holý, A., Wutzler, P. & De Clercq, E.
      Inhibitory effects of novel nucleoside and nucleotide analogues on Epstein-Barr virus replication.
      Antiviral Chem. Chemother., 9: 275-282 (1998).
      


1280. Thormar, H., Georgsson, G., Gunnarsson, E., Naesens, L., Torsteinsdóttir, S., Balzarini, J. & De Clercq, E.
      Treatment of visna virus infection in lambs with the acyclic nucleoside phosphonate analog 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
      Antiviral Chem. Chemother., 9: 245-252 (1998).
      


1281. Vandamme, A.-M., Van Vaerenbergh, K. and De Clercq, E.
      Anti-HIV drug combination strategies.
      Antiviral Chem. Chemother., 9: 187-203 (1998).
      


1282. Ochoa, C., Provencio, R., Jimeno, M.L., Balzarini, J. & De Clercq, E.
      Synthesis and anti-HIV properties of 1,2,4,6-thiatriazin-3-one 1,1-dioxide nucleosides.
      Nucleosides & Nucleotides, 17: 901-910 (1998).
      


1283. Meier, C., Lorey, M., De Clercq, E. & Balzarini, J.
      CycloSal-2’,3’-dideoxy-2’,3’-didehydrothymidine monophosphate (cycloSal-d4TMP): synthesis and antiviral evaluation of a new d4TMP delivery system.
      J. Med. Chem., 41: 1417-1427 (1998).
      


1284. Papakonstantinou-Garoufalias, S., Filippatos, E., Todoulou, O., Tsantili-Kakoulidou, A., Papadaki-Valiraki, A., De Clercq, E. & Lada-Chytiroglou, A.
      Synthesis, lipophilicity and biological properties of some novel 1H-1,2,4 triazole derivatives.
      Il Farmaco, 52: 707-710 (1998).
      


1285. Efimtseva, E.V., Mikhailov, S.N., Fomicheva, M.V., Meshkov, S.V., Rodionov, M.S., Khomutov, A.R. & De Clercq, E.
      Acyclic nucleotide analogues on the basis of phosphonic acids.
      Russian J. Bioorg. Chem., 24: 12-16 (1998).
      Bioorganicheskaya Khimiya, 24: 16-20 (1998).
      


1286. Lazrek, H.B., Rochdi, A., Khaider, H., Barascut, J.-L., Imbach, J.-L., Balzarini, J., Witvrouw, M., Pannecouque, C. & De Clercq, E.
      Synthesis of (Z) and (E) -alkenyl phosphonic acid derivatives of purines and pyrimidines.
      Tetrahedron, 54: 3807-3816 (1998).
      


1287. De Clercq, E.
      New perspectives for the treatment of HIV infections.
      Verh. K. Acad. Geneesk. Belg., 60: 13-45 (1998).
      


1288. De Clercq, E.
      Treatment strategy for HIV infection: hit early, hit hard, and hit long.
      Current Anti-Infective Therapy, 18: 4-5 (1998).
      


1289. Hatse, S., Naesens, L., Degrève, B., Segers, C., Vandeputte, M., Waer, M., De Clercq, E. & Balzarini, J.
      Potent antitumor activity of the acyclic nucleoside phosphonate 9-(2-phosphonyl-methoxyethyl)adenine in choriocarcinoma-bearing rats.
      Int. J. Cancer, 76: 595-600 (1998).
      


1290. Balzarini, J., Degrève, B., Andrei, G., Neyts, J., Sandvold, M., Myhren, F. & De Clercq, E.
      Superior cytostatic actvity of the ganciclovir elaidic ester due to the prolonged intracellular retention of ganciclovir anabolites in herpes simplex virus type 1 thymidine kinase gene-transfected tumor cells.
      Gene Ther., 5: 419-426 (1998).
      


1291. Schols, D., Esté, J.A., Cabrera, C. & De Clercq, E.
      T-cell-line-tropic human immunodeficiency virus type 1 that is made resistant to stromal cell-derived factor 1 contains mutations in the envelope gp120 but does not show a switch in coreceptor use.
      J. Virol., 72: 4032-4037 (1998).
      


1292. Debyser, Z., Van Wijngaerden, E., Van Laethem, K.,Beuselinck, K., Reynders, M., De Clercq, E., Desmyter, J. & Vandamme, A.-M.
      Failure to quantify viral load with two of the three commercial methods in a pregnant woman harboring an HIV type 1 subtype G strain.
      AIDS Res. Human Retroviruses, 14: 453-459 (1998).
      


1293. Annaert, P., Gosselin, G., Pompon, A., Benzaria, S., Valette, G., Imbach, J.-L., Naesens, L., Hatse, S., De Clercq, E., Van den Mooter, G., Kinget, R. & Augustijns, P.
      Comparison of the disposition of ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA in Caco-2 monolayers
      Pharm. Res., 15: 239-245 (1998).
      


1294. Balzarini, J., Hatse, S., Naesens, L. & De Clercq, E.
      Selection and characterisation of murine leukaemia L1210 cells with high-level resistance to the cytostatic activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxy-ethyl)adenine (PMEA).
      Biochim. Biophys. Acta, 1402: 29-38 (1998).
      


1295. Balzarini, J., Cahard, D., Wedgwood, O., Salgado, A., Velázquez, S., Yarnold, C.J., De Clercq, E., McGuigan, C. & Thormar, H.
      Marked inhibitory activity of masked aryloxy aminoacyl phosphoramidate derivatives of dideoxynucleoside analogues against visna virus infection.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 17: 296-302 (1998).
      


1296. Dimmock, J.R., Kandepu, N.M., Hetherington, M., Quail, J.W., Pugazhenthi, U., Sudom, A.M., Chamankhah, M., Rose, P., Pass, E., Allen, T.M., Halleran, S., Szydlowski, J., Mutus, B., Tannous, M., Manavathu, E.K., Myers, T.G., De Clercq, E. & Balzarini, J.
      Cytotoxic activities of Mannich bases of chalcones and related compounds.
      J. Med. Chem., 41: 1014-1026 (1998).
      


1297. Wu, J., Schneller, S.W., Seley, K.L. & De Clercq, E.
      Carbocyclic 7-deazaguanine oxetanocin analogues.
      Heterocycles, 47: 757-763 (1998).
      


1298. Proost, P., De Meester, I., Schols, D., Struyf, S., Lambeir, A..-M., Wuyts, A., Opdenakker, G., De Clercq, E., Scharpé, S. & Van Damme, J.
      Amino-terminal truncation of chemokines by CD26/dipeptidyl peptidase IV. Conversion of RANTES into a potent inhibitor of monocyte chemotaxis and HIV-1-infection.
      J. Biol. Chem., 273: 7222-7227 (1998).
      


1299. De Clercq, E.
      Carbocyclic adenosine analogues as S-adenosylhomocysteine hydrolase inhibitors and antiviral agents: recent advances.
      Nucleosides & Nucleotides, 17: 625-634 (1998).
      


1300. Daelemans, D., Vandamme, A.-M., Shuto, S., Matsuda, A. & De Clercq, E.
      Stereospecificity of 6’-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.
      Nucleosides & Nucleotides, 17: 479-486 (1998).
      


1301. Snoeck, R., Wellens, W., Desloovere, C., Van Ranst, M., Naesens, L., De Clercq, E. & Feenstra, L.
      Treatment of severe laryngeal papillomatosis with intralesional injections of cidofovir [(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine].
      J. Med. Virol., 54: 219-225 (1998).
      


1302. Witvrouw, M., Arranz, M.E., Pannecouque, C., Declercq, R., Jonckheere, H., Schmit, J.-C., Vandamme, A.-M., Diaz, J.A., Ingate, S.T., Desmyter, J., Esnouf, R., Van Meervelt, L., Vega, S., Balzarini, J. & De Clercq, E.
      1,1,3-Trioxo-2H,4H-thieno[3,4-e[1,2,4thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors (NNRTIs) with anti-HIV-1 activity.
      Antimicrob. Agents Chemother., 42: 618-623 (1998).
      


1303. Esté, J.A., Cabrera, C., Schols, D., Cherepanov, P., Gutierrez, A., Witvrouw, M., Pannecouque, C., Debyser, Z., Rando, R.F., Clotet, B., Desmyter, J. & De Clercq, E.
      Human immunodeficiency virus glycoprotein gp120 as the primary target for the antiviral action of AR177 (zintevir).
      Mol. Pharmacol., 53: 340-345 (1998).
      


1304. McGuigan, C., Tsang, H.-W., De Clercq, E. & Balzarini, J.
      Synthesis and anti-HIV activity of some novel chain-extended phosphoramidate derivatives of d4T (stavudine): esterase hydrolysis as a rapid predictive test for antiviral potency.
      Antiviral Chem. Chemother., 9: 109-115 (1998).
      


1305. Neyts, J., Sadler, R., De Clercq, E., Raab-Traub, N. & Pagano, J.S.
      The antiviral agent cidofovir [(S)-1-(3-hydroxy-2-phosphonyl-methoxypropyl)cytosine has pronounced activity against nasopharyngeal carcinoma grown in nude mice.
      Cancer Res., 58: 384-388 (1998).
      


1306. Balzarini, J., Pelemans, H., Riess, G., Roesner, M., Winkler, I., De Clercq, E. & Kleim, J.-P.
      Retention of marked sensitivity to (S)-4-isopropoxycarbonyl-6-methoxy-3-(methylthiomethyl)-3,4-dihydroquinoxaline-2(1H)-thione (HBY 097) by an azido-thymidine (AZT)-resistant human immunodeficiency virus type 1 (HIV-1) strain subcultured in the combined presence of quinoxaline HBY 097 and 2’,3’-dideoxy-3’-thiacytidine (lamivudine).
      Biochem. Pharmacol., 55: 617-625 (1998).
      


1307. Hartmann, K., Kuffer, M., Balzarini, J., Naesens, L., Goldberg, M., Erfle, V., Goebel, F.-D., De Clercq, E., Jindrich, J., Holý, A., Bischofberger, N. & Kraft, W.
      Efficacy of the acyclic nucleoside phosphonates (S)-9-(3-fluoro-2-phosphonylmethoxy­propyl)adenine (FPMPA) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against feline immunodeficiency virus.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 17: 120-128 (1998).
      


1308. Balzarini, J., Pelemans, H., Esnouf, R. & De Clercq, E.
      A novel mutation (F227L) arises in the reverse transcriptase of human immunodeficiency virus type 1 on dose-escalating treatment of HIV type 1-infected cell cultures with the nonnucleoside reverse transcriptase inhibitor thiocarboxanilide UC-781.
      AIDS Res. Hum. Retroviruses, 14: 255-260 (1998).
      


1309. Jonckheere, H., Witvrouw, M., Desmyter, J., De Clercq, E. & Anné, J.
      Lamivudine resistance of HIV type 1 does not delay development of resistance to nonnucleoside HIV type 1-specific reverse transcriptase inhibitors as compared to the wild type HIV type 1.
      AIDS Res. Hum. Retroviruses, 14: 249-253 (1998)
      


1310. De Clercq, E.
      Acyclic nucleoside phosphonates: a new dimension to the chemotherapy of DNA virus and retrovirus infections.
      J. Med. Microbiol., 47: 1-3 (1998).
      


1311. Balzarini, J., Degrève, B. & De Clercq, E.
      Improving AZT efficacy (Letter).
      Nature Medicine, 4: 132 (1998).
      


1312. Neyts, J., Andrei, G. & De Clercq, E.
      The novel immunosuppressive agent Mycophenolate Mofetil markedly potentiates the antiherpes virus activities of acyclovir, ganciclovir and penciclovir in vitro and in vivo.
      Antimicrob. Agents Chemother., 42: 216-222 (1998).
      


1313. Neyts, J., Balzarini, J., Andrei, G., Chaoyong, Z., Snoeck, R., Zimmerman, A., Mertens, T., Karlsson, A. & De Clercq, E.
      Intracellular metabolism of the N7-substituted acyclic nucleoside analog 2-amino-7-(1,3-dihydroxy-2-propoxymethyl)purine, a potent inhibitor of herpesvirus replication.
      Mol. Pharmacol., 53: 157-165 (1998).
      


1314. Revankar, G.R., Ojwang, J.O., Mustain, S.D., Rando, R.F., De Clercq, E., Huffman, J.H., Drach, J.C., Sommadossi, J.-P. & Lewis, A.F.
      Thiazolo[4,5-d]pyrimidines. Part II. Synthesis and anti-human cytomegalovirus (HCMV) activity in vitro of certain acyclonucleosides and acyclonucleotides derived from the guanine analogue 5-aminothiazolo[4,5-d]pyrimidine-2,7(3H,6H)-dione.
      Antiviral Chem. Chemother., 9: 53-63 (1998).
      


1315. Donzella, G.A., Schols, D., Lin, S.W., Esté, J.A., Nagashima, K.A., Maddon, P.J., Allaway, G.P., Sakmar, T.P., Henson, G., De Clercq, E. & Moore, J.P.
      AMD3100, a small-molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor
      Nature Medicine, 4: 72-77 (1998).
      


1316. Neyts, J. & De Clercq, E.
      In vitro and in vivo inhibition of murine gamma herpesvirus 68 replication by selected antiviral agents.
      Antimicrob. Agents Chemother., 42: 170-172 (1998).
      


1317. De Clercq, E.
      Brivudin (BVDU): Wirkspektrum und Mechanismus der antiviralen Aktivität.
      Konsensuskonferenz zur Antiviralen Chemotherapie des Herpes Zoster, P. Wutzler and H.W. Doerr (eds.), Paul-Ehrlich-Gesellschaft für Chemotherapie, Erfurt, 17-19 March, 1997
      Veröffentlichung des Konsensuspapieres: Chemotherapie Journal, 6: 134-135 (1997); Deutsches Ärzteblatt, 95: 2-4 (1998).
      



87 publications in the year 1997



1318. De Clercq, E.
      Non-nucleoside reverse transcriptase inhibitors: an overview.
      In: “Insight in HIV Disease Management”, Issue 6:1, C.S. Crumpacker (ed.). Meniscus Health Care Communications, Bala Cynwyd, Pennsylvania, USA, pp. 2-9 (1997).
      


1319. Balo, C., Fernández, F., Lens, E., López, C., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Novel carbocyclic nucleosides containing a cyclopentyl ring. Adenosine and uridine analogues.
      Arch. Pharm. Pharm. Med. Chem., 330: 265-267 (1997).
      


1320. Manfredini, S., Baraldi, P.G., Bazzanini, R., Simoni, D., Balzarini, J. & De Clercq, E.
      Synthesis and antiproliferative activity of 2’-O-allyl-1--D-arabinofuranosyl-uracil, -cytosine and -adenine.
      Bioorg. Med. Chem. Lett., 7: 473-478 (1997).
      


1321. De Clercq, E.
      Acyclic nucleoside phosphonates in the chemotherapy of DNA virus and retrovirus infections.
      Proceedings “Perspectiven der Therapie von Virusinfektionen”, Berlin, Germany, 10-11 October 1997.
      Intervirology, 40: 295-303 (1997).
      


1322. Kundu, N.G., Das, P., Balzarini, J. & De Clercq, E.
      Palladium-catalyzed synthesis of [E-6-(2-acetylvinyl)uracils and [E-6-(2-acylvinyl)-1-[(2-hydroxyethoxy)methyluracils - their antiviral and cytotoxic activities.
      Bioorg. Med. Chem., 5: 2011-2018 (1997).
      


1323. Van Maarseveen, J.H., Scheeren, H.W. De Clercq, E., Balzarini, J. & Kruse, C.G.
      Antiviral and tumor cell antiproliferative SAR studies on tetracyclic Eudistomins. II.
      Bioorg. Med. Chem., 5: 955-970 (1997).
      


1324. Taskintuna, I., Rahhal, F.M., Rao, N.A., Wiley, C.A., Mueller, A.J., Banker, A.S., De Clercq, E., Arevalo, J.F. & Freeman, W.R.
      Adverse events and autopsy findings after intravitreous cidofovir (HPMPC) therapy in patients with acquired immune deficiency syndrome (AIDS).
      Ophthalmology, 104: 1827-1837 (1997).
      


1325. Wellens, W., Snoeck, R., Desloovere, C., Van Ranst, M., Naesens, L., De Clercq, E. & Feenstra, L.
      Treatment of severe laryngeal papillomatosis with intralesional injections of Cidofovir [(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, HPMPC, Vistide.
      Proceedings of the XVI World Congress of Otorhinolaryngology Head and Neck Surgery, Sydney, Australia, 2-7 March 1997. G. McCafferty, W. Coman & R. Carroll (eds.), Monduzzi Editore, Bologna, Italy, pp. 455-459 (1997).
      


1326. Chavez-de la Paz, E., Arevalo, J.F., Kirsch, L.S., Munguia, D., Rahhal, F.M., De Clercq, E. & Freeman, W.R.
      Anterior nongranulomatous uveitis after intravitreal HPMPC (cidofovir) for the treatment of cytomegalovirus retinitis.
      Ophthalmology, 104: 539-544 (1997).
      


1327. Van Derpoorten, K., Balzarini, J., De Clercq, E. & Poupaert, J.H.
      Anti-HIV activity of N-1-adamantyl-4-aminophthalimide.
      Biomed. & Pharmacother., 51: 464-469 (1997).
      


1328. Fytas, G., Stamatiou, G., Foscolos, G.B., Kolocouris, A., Kolocouris, N., Witvrouw, M., Pannecouque, C. & De Clercq, E.
      Synthesis and anti-HIV activity of some new aminoadamantane heterocycles.
      Bioorg. Med. Chem. Lett., 7: 1887-1890 (1997).
      


1329. Daelemans, D., Esté, J.A., Witvrouw, M., Pannecouque, C., Jonckheere, H., Aquaro, S., Perno, C.-F., De Clercq, E. & Vandamme, A.-M.
      S-Adenosylhomocysteine hydrolase inhibitors interfere with the replication of human immunodeficiency virus type 1 through inhibition of the LTR transactivation.
      Mol. Pharmacol., 52: 1157-1163 (1997).
      


1330. Neyts, J. & De Clercq, E.
      Antiviral drug susceptibility of human herpesvirus 8.
      Antimicrob. Agents Chemother., 41: 2754-2756 (1997).
      


1331. De Vreese, K., Van Nerum, I., Vermeire, K., Anné, J. & De Clercq, E.
      Sensitivity of human immunodeficiency virus to bicyclam derivatives is influenced by the three-dimensional structure of gp120.
      Antimicrob. Agents Chemother., 41: 2616-2620 (1997).
      


1332. Ingate, S.T., Marco, J.L., Witvrouw, M., Pannecouque, C. & De Clercq, E.
      Studies into the synthesis of derivatives of 4-amino-2,3-dihydroisothiazole 1,1-dioxides and 4-amino-1,2-oxathiole 2,2-dioxides: the search for linked -system containing analogues as potential inhibitors of HIV-1 reverse transcriptase.
      Tetrahedron, 53: 17795-17814 (1997).
      


1333. Santana, L., Teijeira, M., Uriarte, E., Terán, C., Andrei, G., Snoeck, R. & De Clercq, E.
      Synthesis and biological activity of some 2-aminopurine carbonucleosides.
      Proceedings of the XIIth International Round Table on Nucleosides, Nucleotides and their Biological Applications, La Jolla, California, U.S.A., September 15-19, 1996.
      Nucleosides & Nucleotides, 16: 1337-1339 (1997).
      


1334. Lorey, M., Meier, C., De Clercq, E. & Balzarini, J.
      Cyclo-saligenyl-5-fluoro-2’-deoxyuridine monophosphate (cycloSal-FdUMP) – a new prodrug approach for FdUMP.
      Proceedings of the XIIth International Round Table on Nucleosides, Nucleotides and their Biological Applications, La Jolla, California, U.S.A., September 15-19, 1996.
      Nucleosides & Nucleotides, 16: 1307-1310 (1997).
      


1335. Meier, C., Lorey, M., De Clercq, E. & Balzarini, J.
      Cyclo-saligenyl-2’,3’-dideoxy-2’,3’-didehydrothymidine monophosphate (cycloSal-d4TMP) – a new pro-nucleotide approach.
      Proceedings of the XIIth International Round Table on Nucleosides, Nucleotides and their Biological Applications, La Jolla, California, U.S.A., September 15-19, 1996.
      Nucleosides & Nucleotides, 16: 1303-1306 (1997).
      


1336. Poopeiko, N.E., Khripach, N.B., Kazimierczuk, Z., Balzarini, J., De Clercq, E. & Mikhailopulo, I.A.
      Synthesis and biological evaluation of 2’,3’-dideoxy-3’-fluororibofuranosyl purine nucleosides.
      Proceedings of the XIIth International Round Table on Nucleosides, Nucleotides and their Biological Applications, La Jolla, California, U.S.A., September 15-19, 1996.
      Nucleosides & Nucleotides, 16: 1083-1086 (1997).
      


1337. Alvarez, R., Jimeno, M.-L., De Clercq, E., Balzarini, J. & Camarasa, M.-J.
      Novel analogues of the anti-HIV-1 agent TSAO-T modified at the 3’-spiro moiety.
      Proceedings of the XIIth International Round Table on Nucleosides, Nucleotides and their Biological Applications, La Jolla, California, U.S.A., September 15-19, 1996.
      Nucleosides & Nucleotides, 16: 1033-1036 (1997).
      


1338. Naesens, L. & De Clercq, E.
      Therapeutic potential of HPMPC (cidofovir), PMEA (adefovir) and related acyclic nucleoside phosphonate analogues as broad-spectrum antiviral agents.
      Proceedings of the XIIth International Round Table on Nucleosides, Nucleotides and their Biological Applications, La Jolla, California, U.S.A., September 15-19, 1996.
      Nucleosides & Nucleotides, 16: 983-992 (1997).
      


1339. Cherepanov, P., Esté, J.A., Rando, R.F., Ojwang, J.O., Reekmans, G., Steinfeld, R., David, G., De Clercq, E. & Debyser, Z.
      Mode of interaction of G-quartets with the integrase of human immunodeficiency virus type 1.
      Mol. Pharmacol., 52: 771-780 (1997).
      


1340. Manfredini, S., Simoni, D., Ferroni, R., Bazzanini, R., Vertuani, S., Hatse, S., Balzarini, J. & De Clercq, E.
      Retinoic acid conjugates as potential antitumor agents: synthesis and biological activity of conjugates with ara-A, ara-C, the 3(2H)-furanone, and aniline mustard moieties.
      J. Med. Chem., 40: 3851-3857 (1997).
      


1341. McGuigan, C., Velázquez, S., De Clercq, E. & Balzarini, J.
      Synthesis and evaluation of 5-halo 2’,3’-didehydro-2’,3’-dideoxynucleosides and their blocked phosphoramidates as potential anti-human immunodeficiency virus agents: an example of ‘kinase bypass’.
      Antiviral Chem. Chemother., 8: 519-527 (1997).
      


1342. Alvarez, R., Jimeno, M.-L., Pérez-Pérez, M.-J., De Clercq, E., Balzarini, J. & Camarasa, M.-J.
      Synthesis, anti-human immunodeficiency virus type 1 activity of novel 3’-spiro nucleosides analogues of TSAO-T.
      Antiviral Chem. Chemother., 8: 507-517 (1997).
      


1343. Pelemans, H., Esnouf, R., Dunkler, A., Parniak, M.A., Vandamme, A.-M., Karlsson, A., De Clercq, E., Kleim, J.-P. & Balzarini, J.
      Characteristics of the Pro225His mutation in human immunodeficiency virus type 1 (HIV-1) reverse transcriptase that appears under selective pressure of dose-escalating quinoxaline treatment of HIV-1.
      J. Virol., 71: 8195-8203 (1997).
      


1344. De Clercq, E.
      Nieuwe perspectieven voor de behandeling van HIV infecties: Is er met de nieuwe behandelingsmethoden een genezing van AIDS in het verschiet ?
      Proceedings, Koninklijke Nederlandse Akademie van Wetenschappen, Afdeling Natuurkunde, deel 106, nr. 8, pp. 107-110 (1997).
      


1345. Balzarini, J., Pelemans, H., Riess, G., Roesner, M., Winkler, I., De Clercq, E. & Kleim, J.-P.
      Zidovudine-resistant human immunodeficiency virus type 1 strains subcultured in the presence of both lamivudine and quinoxaline HBY 097 retain marked sensitivity to HBY 097 but not to lamivudine.
      J. Infect. Dis., 176: 1392-1397 (1997).
      


1346. Degrève, B., Andrei, G., Izquierdo, M., Piette, J., Morin, K., Knaus, E.E., Wiebe, L.I., Basrah, I., Walker, R.T., De Clercq, E. & Balzarini, J.
      Varicella-zoster virus thymidine kinase gene and antiherpetic pyrimidine nucleoside analogues in a combined gene/chemotherapy treatment for cancer.
      Gene Therapy, 4: 1107-1114 (1997).
      


1347. Molina, S., Cobo, J., Melguizo, M., Nogueras, M., Sánchez, A., Ortiz, A. & De Clercq, E.
      Synthesis and antiviral activity of several 6-(methylenecarbomethoxy)pteridin-4,7(3H,8H)-diones.
      In: “Chemistry and Biology of Pteridines and Folates 1997”, W. Pfleiderere & H. Rokos (eds.), Proceedings of the Eleventh International Symposium on Pfteridines and Folates, Berchtesgaden, Germany, 15-20 June 1997. Blackwell Science, Berlin, pp. 57-60 (1997).
      


1348. Witvrouw, M. & De Clercq, E.
      Review: Sulfated polysaccharides extracted from sea algae as potential antiviral drugs.
      Gen. Pharmacol., 29: 497-511 (1997).
      


1349. Schols, D., Struyf, S., Van Damme, J., Esté, J.A., Henson, G. & De Clercq, E.
      Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4.
      J. Exp. Med., 186: 1383-1388 (1997).
      


1350. De Clercq, E.
      In search of a selective antiviral chemotherapy.
      Clin. Microbiol. Rev., 10: 674-693 (1997).
      


1351. De Clercq, E.
      Virus replication: target functions and events for virus-specific inhibitors.
      In: "Antiviral Agents and Human Viral Diseases", 4th ed., G.J. Galasso, R.J. Whitley & T.C. Merigan (eds.). Lippincott-Raven Publishers, Philadelphia, pp. 1-44 (1997).
      


1352. Wnuk, S.F., Yuan, C.-S., Borchardt, R.T., Balzarini, J., De Clercq, E. & Robins, M.J.
      Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5’-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues.
      J. Med. Chem., 40: 1608-1618 (1997).
      


1353. Seley, K.L., Schneller, S.W. & De Clercq, E.
      A methylated derivative of 5’-noraristeromycin.
      J. Org. Chem., 62: 5645-5646 (1997).
      


1354. Andrei, G., Snoeck, R. & De Clercq, E.
      Differential susceptibility of several drug-resistant strains of herpes simplex virus type 2 to various antiviral compounds.
      Antiviral Chem. Chemother., 8: 457-461 (1997).
      


1355. Dimmock, J.R., Erciyas, E., Kumar, P., Hetherington, M., Quail, J.W., Pugazhenthi, U., Arpin, S.A., Hayes, S.J., Allen, T.M., Halleran, S., De Clercq, E., Balzarini, J. & Stables, J.P.
      Mannich bases of phenolic azobenzenes possessing cytotoxic activity.
      Eur. J. Med. Chem., 32: 583-594 (1997).
      


1356. Liekens, S., Neyts, J., Degrève, B. & De Clercq, E.
      The sulfonic acid polymers PAMPS [poly(2-acrylamido-2-methyl-1-propanesulfonic acid) and related analogues are highly potent inhibitors of angiogenesis.
      Oncol. Res., 9: 173-181 (1997)
      


1357. Schols, D., Proost, P., Van Damme, J. & De Clercq, E.
      RANTES and MCP-3 inhibit the replication of T-cell-tropic human immunodeficiency virus type 1 strains (SF-2, MN, and HE).
      J. Virol., 71: 7300-7304 (1997).
      


1358. Zimmermann, A., Michel, D., Pavic, I., Hampl, W., Lüske, A., Neyts, J., De Clercq, E. & Mertens, T.
      Phosphorylation of aciclovir, ganciclovir, penciclovir and S2242 by the cytomegalovirus UL97 protein: a quantitative analysis using recombinant vaccinia viruses.
      Antiviral Res., 36: 35-42 (1997).
      


1359. Meier, C., De Clercq, E. & Balzarini, J.
      Cyclo-saligenyl-3’-azido-2’,3’-dideoxythymidinemonophosphate (cycloSal-AZTMP) - a new pro-nucleotide approach ?
      Nucleosides & Nucleotides, 16: 793-796 (1997).
      


1360. Lorey, M., Meier, C., De Clercq, E. & Balzarini, J.
      New synthesis and antitumor activity of cycloSal-derivatives of 5-fluoro-2’-deoxyuridinemonophosphate.
      Nucleosides & Nucleotides, 16: 789-792 (1997).
      


1361. McGuigan, C., Tsang, H.-W., Cahard, D., Turner, K., Velázquez, S., Salgado, A., Bidois, L., Naesens, L., De Clercq, E. & Balzarini, J.
      Phosphoramidate derivatives of d4T as inhibitors of HIV: the effect of amino acid variation.
      Antiviral Res., 35: 195-204 (1997).
      


1362. Schols, D., Esté, J.A., Henson, G. & De Clercq, E.
      Bicyclams, a class of potent anti-HIV agents, are targeted at the HIV coreceptor fusin/CXCR-4.
      Antiviral Res., 35: 147-156 (1997).
      


1363. Banker, A.S., Arevalo, J.F., Munguia, D., Rahhal, F.M., Ishimoto, B., Berry, C., De Clercq, E., Ochabski, R., Taskintuna, I. & Freeman, W.R.
      Intraocular pressure and aqueous humor dynamics in patients with AIDS treated with intravitreal cidofovir (HPMPC) for cytomegalovirus retinitis.
      Am. J. Ophthalmol., 124: 168-180 (1997).
      


1364. Maurinsh, Y., Schraml, J., De Winter, H., Blaton, N., Peeters, O., Lescrinier, E., Rozenski, J., Van Aerschot, A., De Clercq, E., Busson, R. & Herdewijn, P.
      Synthesis and conformational study of 3-hydroxy-4-’hydroxymethyl)-1-cyclohexanyl purines and pyrimidines.
      J. Org. Chem., 62: 2861-2871 (1997).
      


1365. Meier, C., Knispel, T., De Clercq, E. & Balzarini, J.
      ADA-Bypass by lipophilic cycloSa1-ddAMP pro-nucleotides - a second example of the efficiency of the cycloSa1-concept.
      Bioorg. Med. Chem. Lett., 7: 1577-1582 (1997).
      


1366. Taskintuna, I., Banker, A.S., Rao, N.A., Wiley, C.A., Flores-Aguilar, M., Munguia, D., Bergeron-Lynn, G., De Clercq, E., Keefe, K. & Freeman, W.R.
      An animal model for cidofovir (HPMPC) toxicity: intraocular pressure and histopa­thologic effects.
      Exp. Eye Res., 64: 795-806 (1997).
      


1367. De Clercq, E.
      Development of resistance of human immunodeficiency virus (HIV) to anti-HIV agents: how to prevent the problem ?
      Int. J. Antimicrob. Agents, 9: 21-36 (1997).
      


1368. Balzarini, J., Kruining, J., Wedgwood, O., Pannecouque, C., Aquaro, S., Perno, C.-F., Naesens, L., Witvrouw, M., Heijtink, R., De Clercq, E. & McGuigan, C.
      Conversion of 2’,3’-dideoxyadenosine (ddA) and 2’,3’-didehydro-2’,3’-dideoxy-adenosine (d4A) to their corresponding aryloxyphosphoramidate derivatives markedly potentiates their activity against human immunodeficiency virus and hepatitis B virus.
      FEBS Lett., 410: 324-328 (1997).
      


1369. Esté, J.A., Schols, D., De Vreese, K., Van Laethem, K., Vandamme, A.-M., Desmyter, J. & De Clercq, E.
      Development of resistance of human immunodeficiency virus type 1 to dextran sulfate associated with the emergence of specific mutations in the envelope gp120 glycoprotein.
      Mol. Pharmacol., 52: 98-104 (1997).
      


1370. Balzarini, J., De Clercq, E. & Überla, K.
      SIV/HIV-1 hybrid virus expressing the reverse transcriptase gene of HIV-1 remains sensitive to HIV-1-specific reverse transcriptase inhibitors after passage in rhesus macaques.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 15: 1-4 (1997).
      


1371. Shuto, S., Obara, T., Saito, Y., Yamashita, K., Tanaka, M., Sasaki, T., Andrei, G., Snoeck, R., Neyts, J., Padalko, E., Balzarini, J., De Clercq, E. & Matsuda, A.
      New neplanocin analogues. VIII. Synthesis and biological activity of 6'-C-ethyl, -ethenyl, and -ethynyl derivatives of neplanocin A.
      Chem. Pharm. Bull, 45: 1163-1168 (1997).
      


1372. De Clercq, E.
      Antiviral metal complexes.
      Metal-Based Drugs, 4: 173-192 (1997).
      


1373. Witvrouw, M., Pannecouque, C. & De Clercq, E.
      Polysulfates: chemistry and potential as antiviral drugs.
      In: "Carbohydrates in Drug Design", Z.J. Witczak & K.A. Nieforth (eds.), Marcel Dekker, Inc., New York, pp. 157-207 (1997).
      


1374. Chimirri, A., Grasso, S., Molica, C., Monforte, A.-M., Monforte, P., Zappalà, M., Bruno, G., Nicolò, F., Witvrouw, M., Jonckheere, H., Balzarini, J. & De Clercq, E.
      Structural features and anti-human immunodeficiency virus (HIV) activity of the isomers of 1-(2’,6’-difluorophenyl)-1H,3H-thiazolo[3,4-abenzimidazole, a potent non-nucleoside HIV-1 reverse transcriptase inhibitor.
      Antiviral Chem. Chemother., 8: 363-370 (1997).
      


1375. Naesens, L. & De Clercq, E.
      New perspectives for the treatment of HIV infection (AIDS).
      Proceedings of the 5th International Symposium on Pharmaceutical Sciences, Ankara, Turkey, 24-27 June 1997.
      J. Fac. Pharm. (Journal of Pharmacy, Ankara, University), pp 180-195 (1997).
      


1376. Esnouf, R.M., Stuart, D.I., De Clercq, E., Schwartz, E. & Balzarini, J.
      Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives.
      Biochem. Biophys. Res. Commun., 234: 458-464 (1997).
      


1377. Cobo, J., Sánchez, A., Nogueras, M. & De Clercq, E.
      Synthesis and antiviral evaluation of pyridine fused heterocyclic and nucleosidic derivatives.
      Tetrahedron, 53: 8225-8236 (1997).
      


1378. Martinez, A., Esteban, A.I. & De Clercq, E.
      Benzothiadiazine dioxides acyclonucleosides as lead compounds for the development of new agents against human cytomegalovirus and varicella-zoster virus infections.
      Bioorg. Med. Chem. Lett., 7: 1031-1032 (1997).
      


1379. Meier, C., Lorey, M., De Clercq, E. & Balzarini, J.
      Cyclic saligenyl phosphotriesters of 2’,3’-dideoxy-2’,3’-didehydrothymidine (d4T) - a new pro-nucleotide approach.
      Bioorg. Med. Chem. Lett., 7: 99-104 (1997).
      


1380. Taskintuna, I., Rahhal, F.M., Arevalo, J.F., Munguia, D., Banker, A.S., De Clercq, E. & Freeman, W.R.
      Low-dose intravitreal cidofovir (HPMPC) therapy of cytomegalovirus retinitis in patients with the acquired immune deficiency syndrome.
      Ophthalmology, 104: 1049-1057 (1997).
      


1381. Dimmock, J.R., Kumar, P., Allen, T.M., Kao, G.Y., Halleran, S., Balzarini, J. & De Clercq, E.
      Synthesis and cytotoxic evaluation of some carbohydrazones and thiocarbohydrazones of various unsaturated ketones and related Mannich bases.
      Pharmazie, 52: 182-186 (1997).
      


1382. Kren, V., Olsovský, P., Havlícek, V., Sedmera, P., Witvrouw, M. & De Clercq, E.
      N-Deoxyribosides of ergot alkaloids: synthesis and biological activity.
      Tetrahedron, 53: 4503-4510 (1997).
      


1383. Wu, J., Schneller, S.W., Seley, K.L., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      Carbocyclic oxetanocins lacking the C-3’ methylene.
      J. Med. Chem., 40: 1401-1406 (1997).
      


1384. Annaert, P., Kinget, R., Naesens, L., De Clercq, E. & Augustijns, P.
      Transport, uptake and metabolism of the bis(pivaloyloxymethyl)-ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine in an in vitro cell culture system of the intestinal mucosa (Caco-2).
      Pharm. Res., 14: 492-496 (1997).
      


1385. Hossain, N., Rozenski, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of the -analogues of 1,5-anhydrohexitol nucleosides (1,5-anhydro-2,3-dideoxy-D-ribohexitol nucleosides).
      J. Org. Chem., 62: 2442-2447 (1997).
      


1386. Esteban, A.I., De Clercq, E. & Martinez, A.
      Synthesis and antiviral activity of modified 1,2,6-thiadiazine dioxide acyclonucleosides.
      Nucleosides & Nucleotides, 16: 265-276 (1997).
      


1387. Balzarini, J. & De Clercq, E.
      The thiocarboxanilides UC-10 and UC-781 have an additive inhibitory effect against human immunodeficiency virus type 1 reverse transcriptase and replication in cell culture when combined with other antiretroviral drugs.
      Antiviral Chem. Chemother., 8: 197-204 (1997).
      


1388. Camarasa, M.-J., Pérez-Pérez, M.-J., Velázquez, S., San-Félix, A., Alvarez, R., Ingate, S., Jimeno, M.-L., De Clercq, E. & Balzarini, J.
      An overview of TSAO-T derivatives, a “peculiar” class of HIV-1 specific RT inhibitors.
      In: “Anti-Infectives. Recent Advances in Chemistry and Structure-Activity Relation­ships”, P.H. Bentley & P.J. O’Hanlon (eds.). The Royal Society of Chemistry, Cam­bridge, pp. 259-268 (1997).
      


1389. McGuigan, C., Cahard, D., Salgado, A., Bidois, L., Velazquez, S., Yarnold, C.J., Turner, K., Sutton, P., Wedgewood, O., Tsang, H.-W., Turner, S.J., Wang, Y., O’Leary, G., Mahmood, N., Hay, A., Balzarini, J. & De Clercq, E.
      Design, synthesis and evaluation of some novel nucleotides as inhibitors of HIV.
      In: “Anti-Infectives. Recent Advances in Chemistry and Structure-Activity Relation­ships”, P.H. Bentley & P.J. O’Hanlon (eds.). The Royal Society of Chemistry, Cam­bridge, pp. 251-258 (1997).
      


1390. Miller, M.J., Darwish, I., Ghosh, A., Ghosh, M., Hansel, J.-G., Hu, J., Niu, C., Ritter, A., Scheidt, K., Süling, C., Sun, S., Zhang, D., Budde, A., De Clercq, E., Leong, S., Malouin, F. & Moellmann, U.
      Design, syntheses and studies of new antibacterial antifungal and antiviral agents.
      In: “Anti-Infectives. Recent Advances in Chemistry and Structure-Activity Relation­ships”, P.H. Bentley & P.J. O’Hanlon (eds.). The Royal Society of Chemistry, Cam­bridge, pp. 116-138 (1997).
      


1391. Song, R., Witvrouw, M., Schols, D., Robert, A., Balzarini, J., De Clercq, E., Bernadou, J. & Meunier, B.
      Anti-HIV activities of anionic metalloporphyrins and related compounds.
      Antiviral Chem. Chemother., 8: 85-97 (1997).
      


1392. Blanco, J.M., Caamano, O., Fernández, F., Gómez, G., Nieto, M.I., Balzarini, J., Padalko, E. & De Clercq, E.
      Synthesis and antiviral and cytostatic activities of carbocyclic nucleosides incorporating a modified cyclopentane ring. 1: Guanosine analogues.
      Nucleosides & Nucleotides, 16: 159-171 (1997).
      


1393. Kren, V., Pískala, A., Sedmera, P., Havlícek, V., Prikrylová, V., Witvrouw, M. & De Clercq, E.
      Synthesis and antiviral evaluation of N-ß-ribosides of ergot alkaloids.
      Nucleosides & Nucleotides, 16: 97-106 (1997).
      


1394. Olsufyeva, E.N., Brusentsov, N.A., Todorova, N., Balzarini, J., De Clercq, E. & Preo­brazhenskaya, M.N.
      Daunorubicin derivatives obtained from daunorubicin and nucleoside dialdehydes.
      Nucleosides & Nucleotides, 16: 87-95 (1997).
      


1395. Balzarini, J., Vahlenkamp, T., Egberink, H., Hartmann, K., Witvrouw, M., Pannecouque, C., Casara, P., Navé, J.-F. & De Clercq, E.
      Antiretroviral activities of acyclic nucleoside phosphonates [9-(2-phosphonylmethoxy­ethyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, (R)-9-(2-phosphonylmethoxypro­pyl)adenine, and MDL 74,968 in cell cultures and murine sarcoma virus-infected new­born NMRI mice.
      Antimicrob. Agents Chemother., 41: 611-616 (1997).
      


1396. Andrei, G., Snoeck, R., Vandeputte, M. & De Clercq, E.
      Activities of various compounds against murine and primate polyomavi­ruses.
      Antimicrob. Agents Chemother., 41: 587-593 (1997).
      


1397. Fedorov, I.I., Kazmina, E.M., Gurskaya, G.V., Jasko, M.V., Zavodnic, V.E., Balzarini, J., De Clercq, E., Faraj, A., Sommadossi, J.-P., Imbach, J.-L. & Gosselin, G.
      Novel 3’-C/N-substituted 2’,3’--D-dideoxynucleosides as potential chemotherapeutic agents. 1. Thymidine derivatives: synthesis, structure, and broad spectrum antiviral properties.
      J. Med. Chem., 40: 486-494 (1997).
      


1398. Leydet, A., Jeantet-Segonds, C., Bouchitté, C., Moullet, C., Boyer, B., Roque, J.P., Witvrouw, M., Esté, J., Snoeck, R., Andrei, G. & De Clercq, E.
      Polyanion inhibitors of human immunodeficiency virus and other viruses. 6. Micelle-like anti-HIV polyanionic compounds based on a carbohydrate core.
      J. Med. Chem., 40: 350-356 (1997).
      


1399. Leydet, A., Barragan, V., Boyer, B., Montéro, J.L., Roque, J.P., Witvrouw, M., Esté, J., Snoeck, R., Andrei, G. & De Clercq, E.
      Polyanion inhibitors of human immunodeficiency virus and other viruses. 5. Telomerized anionic surfactants derived from amino acids.
      J. Med. Chem., 40: 342-349 (1997).
      


1400. Witvrouw, M., Balzarini, J., Pannecouque, C., Jhaumeer-Laulloo, S., Esté, J.A., Schols, D., Cherepanov, P., Schmit, J.-C., Debyser, Z., Vandamme, A.-M., Desmyter, J., Ramadas, S.R. & De Clercq, E.
      SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus.
      Antimicrob. Agents Chemother., 41: 262-268 (1997).
      


1401. Witvrouw, M., Schmit, J.-C., Van Remoortel, B., Daelemans, D., Esté, J.A., Vandamme, A.-M., Desmyter, J. & De Clercq, E.
      Cell type-dependent effect of sodium valproate on human immunodeficiency virus type 1 replication in vitro.
      AIDS Res. Human Retrovirol., 13: 187-192 (1997).
      


1402. Balzarini, J., Pelemans, H., De Clercq, E., Karlsson, A. & Kleim, J.-P.
      Reverse transcriptase fidelity and HIV-1 variation (Technical Comment).
      Science, 275: 229-230 (1997).
      


1403. Takahashi, K., Suzuki, M., Iwata, Y., Shigeta, S., Yamanishi, K. & De Clercq, E.
      Selective activity of various nucleoside and nucleotide analogues against human herpes virus 6 and 7.
      Antiviral Chem. Chemother., 8: 24-31 (1997).
      


1404. Naesens, L., Snoeck, R., Andrei, G., Balzarini, J., Neyts, J. & De Clercq, E.
      HPMPC (cidofovir), PMEA (adefovir) and related acyclic nucleoside phosphonate analogues: a review of their pharmacology and clinical potential in the treatment of viral infections.
      Antiviral Chem. Chemother., 8: 1-23 (1997).
      



94 publications in the year 1996



1405. Dullaert, H., Maudgal, P.C., Leys, A., Dralands, L. & De Clercq, E.
      Bromovinyldeoxyuridine treatment of outer retinal necrosis due to varicella-zoster virus: a case-report.
      Bull. Soc. Belge Ophtalmol., no. 262: 107-113 (1997) (pp 107-113, 1996).
      


1406. Hocek, M., Masojídková, M., Holý, A., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Synthesis of acyclic nucleotide analogues derived from 6-(aminomethyl)purines and purine-6-carboxamidines.
      Collect. Czech. Chem. Commun., 61: 1525-1537 (1996).
      


1407. Ochoa, C., Herrero, A., Provencio, R., Balzarini, J., De Clercq, E., Gómez-Barrio, A., Díaz, R.M. & Nogal, J.J.
      First example of a 4-amino-1,2,4,6-thiatriazine 1,1-dioxide derivative.
      Heterocycles, 43: 2199-2204 (1996).
      


1408. Joos, P.E., Esmans, E.L., Alderweireldt, F.C., De Bruyn, A., Balzarini, J. & De Clercq, E.
      Synthesis, conformation analysis and biological evaluation of 2-(2,3-dideoxy--D-ribofuranosyl)pyridine-4-carboxamide.
      Heterocycles, 43: 287-304 (1996).
      


1409. Andrei, G. & De Clercq, E.
      Quimioterapia de las infecciones virales.
      In "Microbiologia", J.A. Basualdo, C.E. Coto & R. de Torres (eds.). Editorial Atlante Argentina, pp. 616-625 (1996).
      


1410. Bruhn, T., Dürig, J., Kraiselburd, E.N., De Clercq, E., Bruhn, H.-D. & Béress, L.
      Antiviral and anticoagulant activity of polysaccharides from marine brown algae.
      Proceedings of the Satellite Symposium on Marine Pharmacology, Eilat, Israel, 9-11 October 1994.
      In: “Biochemical Aspects of Marine Pharmacology”, P. Lazarovici, M.E. Spira & E. Zlotkin (eds.). Alaken, Inc., Fort Collins, Colorado, pp. 187-208 (1996).
      


1411. Debyser, Z. & De Clercq, E.
      Chemical crosslinking of the subunits of HIV-1 reverse transcriptase.
      Protein Science, 5: 278-286 (1996).
      


1412. Kaminsky, R., Schmid, C., Grether, Y., Holý, A., De Clercq, E., Naesens, L. & Brun, R.
      (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine [(S)-HPMPA]: a purine analogue with trypanocidal activity in vitro and in vivo.
      Trop. Med. Int. Health, 1: 255-263 (1996).
      


1413. Mikhailopulo, I.A., Poopeiko, N.E., Tsvetkova, T.M., Marochkin, A.P., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of 3’-C-branched-3’-deoxy analogues of adenosine.
      Carbohydrate Res., 285: 17-28 (1996).
      


1414. Kodama, E., Igarashi, A., Mori, S., Hashimoto, K.-i., Suzuki, T., De Clercq, E. & Shigeta, S.
      Evaluation of antiherpetic compounds using a gastric cancer cell line: pronounced activity of BVDU against herpes simplex virus replication.
      Microbiol. Immunol., 40: 359-363 (1996).
      


1415. Ruiz, L., Romeu, J., Martínez-Picado, J., Schmit, J.-C., Vandamme, A.-M., Balagué, M., Cabrera, C., Puig, T., Tural, C., Segura, A., Sirera, G., De Clercq, E. & Clotet, B.
      Efficacy of triple combination therapy with zidovudine (ZDV) plus zalcitabine (ddC) plus lamivudine (3TC) versus double (ZDV + 3TC) combination therapy in patients previously treated with ZDV + ddC.
      AIDS, 10: F61-F66 (1996).
      


1416. McGuigan, C., Wedgwood, O.M., De Clercq, E. & Balzarini, J.
      Phosphoramidate derivatives of 2',3'-didehydro-2’,3’-dideoxyadenosine (d4A) have markedly improved anti-HIV potency and selectivity.
      Bioorg. Med. Chem. Lett., 6: 2359-2362 (1996).
      


1417. Balzarini, J. & De Clercq, E.
      Analysis of inhibition of retroviral reverse transcriptase
      In: "Viral Polymerases and Related Proteins", L.C. Kuo, D.B. Olsen & S.S. Carroll (eds.), Methods in Enzymology, vol. 275. J.N. Abelson & M.I. Simon (eds.). Academic Press, San Diego, pp. 472-502 (1996).
      


1418. Debyser, Z. & De Clercq, E.
      Antiviral therapy for HIV infection.
      EOS - J. Immunol. Immunopharmacol., 16: 48-52 (1996).
      


1419. Maruyama, T., Sato, Y., Oto, Y. & De Clercq, E.
      Synthesis and antiviral activity of 6-chloropurine arabinoside and 2’-deoxy-2’-fluoro derivatives.
      Nucleic Acids Symp. Series No. 35: 39-40 (1996).
      


1420. Maruyama, T., Sato, Y., Oto, Y., Takahashi, Y., Snoeck, R., Andrei, G., Witvrouw, M. & De Clercq, E.
      Synthesis and antiviral activity of 6-chloropurine arabinoside and its 2'-deoxy-2'-fluoro derivative.
      Chem. Pharm. Bull., 44: 2331-2334 (1996).
      


1421. Swart, P.J., Kuipers, M.E., Smit, C., Pauwels, R., de Béthune, M.P., De Clercq, E., Meijer, D.K.F. & Huisman, J.G.
      Antiviral effects of milk proteins: acylation results in polyanionic compounds with potent activity against human immunodeficiency virus type 1 and 2 in vitro.
      AIDS Res. Human Retrovir., 12: 769-775 (1996).
      


1422. Joos, P.E., De Groot, A., Esmans, E.L., Alderweireldt, F.C., De Bruyn, A., Balzarini, J. & De Clercq, E.
      Synthesis, conformational analysis and biological evaluation of 2-(5-deoxy--D-ribofuranosyl)pyridine-4-carboxamide.
      Heterocycles, 42: 173-187 (1996).
      


1423. Lagneaux, L., Delforge, A., Snoeck, R., Bosmans, E., Moreau, J.F., Taupin, J.L., De Clercq, E., Stryckmans, P. & Bron, D.
      Human cytomegalovirus increases constitutive production of interleukin-6 and leukemia inhibitory factor by bone marrow stromal cells.
      Blood, 87: 59-66 (1996).
      


1424. Lagneaux, L., Delforge, A., Snoeck, R., Bosmans, E., Schols, D., De Clercq, E., Stryckmans, P. & Bron, D.
      Imbalance in production of cytokines by bone marrow stromal cells following cytomega­lovirus infection.
      J. Infect. Dis., 174: 913-919 (1996).
      


1425. Hatse, S., De Clercq, E. & Balzarini, J.
      Evidence for distinction of the differentiation-inducing activities and cytostatic proper­ties of 9-(2-phosphonylmethoxyethyl)adenine and a variety of differentiation-inducing agents in human erythroleukemia K562 cells.
      Mol. Pharmacol., 50: 1231-1242 (1996).
      


1426. Balzarini, J., Egberinck, H., Hartmann, K., Cahard, D., Vahlenkamp, T., Thormar, H., De Clercq, E. & McGuigan, C.
      Antiretrovirus specificity and intracellular metabolism of 2',3'-didehydro-2',3'-dide­oxythymidine (stavudine) and its 5'-monophosphate triester prodrug So324.
      Mol. Pharmacol., 50: 1207-1213 (1996).
      


1427. Ingate, S., De Clercq, E., Balzarini, J. & Camarasa, M.-J.
      Novel L-lyxo and 5'-deoxy-5’-modified TSAO-T analogs: synthesis and anti-HIV-1 activity.
      Antiviral Res., 32: 149-164 (1996).
      


1428. Balzarini, J., Pelemans, H., Karlsson, A., De Clercq, E. & Kleim, J.-P.
      Concomitant combination therapy for HIV infection preferable over sequential therapy with 3TC and non-nucleoside reverse transcriptase inhibitors.
      Proc. Natl. Acad. Sci. USA, 93: 13152-13157 (1996).
      


1429. Jonckheere, H., De Vreese, K., Debyser, Z., Vandekerckhove, J., Balzarini, J., Desmyter, J., De Clercq, E. & Anné, J.
      A two plasmid co-expression system in Escherichia coli for the production of virion-like reverse transcriptase of the human immunodeficiency virus type 1.
      J. Virol. Methods, 61: 113-125 (1996).
      


1430. Naesens, L. & De Clercq, E.
      Present status of HIV protease inhibitors in the control of HIV infections. Introductory Article "Anti-infectives"
      Exp. Opin. Invest. Drugs, 5: 153-154 (1996).
      


1431. De Clercq, E.
      Perspectives for the chemotherapy of respiratory syncytial virus (RSV) infections.
      Int. J. Antimicrobial Agents, 7: 193-202 (1996).
      


1432. Vandamme, A.-M., Schmit, J.-C., Van Dooren, S., Van Laethem, K., Gobbers, E., Kok, W., Goubau, P., Witvrouw, M., Peetermans, W., De Clercq, E. & Desmyter, J.
      Quantification of HIV-1 RNA in plasma: comparable results with the NASBA HIV monitor test.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 13: 127-139 (1996).
      


1433. Schmit, J.-C., Cogniaux, J., Hermans, P., Van Vaeck, C., Sprecher, S., Van Remoortel, B., Witvrouw, M., Balzarini, J., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Multiple drug resistance to nucleoside analogues and nonnucleoside reverse transcrip­tase inhibitors in an efficiently replicating human immunodeficiency virus type 1 patient strain.
      J. Infect. Dis., 174: 962-968 (1996).
      


1434. Mager, P.P., De Clercq, E., Takashima, H., Ubasawa, M., Sekiya, K., Baba, M. & Walther, H.
      Molecular simulation of 5,6-substituted 1-[(2-hydroxyethoxy)methyl]uracils with anti-HIV-1 activity
      Eur. J. Med. Chem., 31: 701-712 (1996).
      


1435. Holý, A., Dvoráková, H., Jindrich, J., Masojídková, M., Budesínský, M., Balzarini, J., Andrei, G. & De Clercq, E.
      Acyclic nucleotide analogs derived from 8-azapurines: synthesis and antiviral activity.
      J. Med. Chem., 39: 4073-4088 (1996).
      


1436. Hossain, N., Rozenski, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of acyclic analogues of 1,5-anhydrohexitol nucleosides using Mitsunobu reaction.
      Tetrahedron, 52: 13655-13670 (1996).
      


1437. Obara, T., Shuto, S., Saito, Y., Snoeck, R., Andrei, G., Balzarini, J., De Clercq, E. & Matsuda, A.
      New neplanocin analogues. 7. Synthesis and antiviral activity of 2-halo derivatives of neplanocin A.
      J. Med. Chem., 39: 3847-3852 (1996).
      


1438. Balo, M.C., Fernández, F., Lens, E., López, C., De Clercq, E., Andrei, G., Snoeck, R. & Balzarini, J.
      Synthesis and antiviral activities of some novel carbocyclic nucleosides.
      Nucleosides & Nucleotides, 15: 1335-1346 (1996).
      


1439. Mikhailov, S.N., De Clercq, E. & Herdewijn, P.
      Ribosylation of pyrimidine 2'-deoxynucleosides.
      Nucleosides & Nucleotides, 15: 1323-1334 (1996).
      


1440. Tsotinis, A., Calogeropoulou, T., Koufaki, M., Souli, C., Balzarini, J., De Clercq, E. & Makriyannis, A.,
      Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3’-azido-3’-deoxythymidine.
      J. Med. Chem., 39: 3418-3422 (1996).
      


1441. Kolocouris, N., Kolocouris, A., Foscolos, G.B., Fytas, G., Neyts, J., Padalko, E., Balzarini, J., Snoeck, R., Andrei, G. & De Clercq, E.
      Synthesis and antiviral activity evaluation of some new aminoadamantane derivatives. 2.
      J. Med. Chem., 39: 3307-3318 (1996).
      


1442. Luyten, I., De Winter, H., Busson, R., Lescrinier, T., Creuven, I., Durant, F., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis of 2’-deoxy-5-(isothiazol-5-yl)uridine and its interaction with the HSV-1 thymidine kinase.
      Helv. Chim. Acta, 79: 1462-1474 (1996).
      


1443. Curic, M., Tusek-Bozic, Lj., Vikic-Topic, D., Scarcia, V., Furlani, A., Balzarini, J. & De Clercq, E.
      Palladium(II) complexes of dialkyl -anilinobenzylphosphonates. Synthesis, characteri­zation, and cytostatic activity.
      J. Inorg. Biochem., 63: 125-142 (1996).
      


1444. Dvoráková, H., Masojídková, M., Holý, A., Balzarini, J., Andrei, G., Snoeck, R. & De Clercq, E.
      Synthesis of 2'-aminomethyl derivatives of N-(2(phosphonomethoxy)ethyl) nucleotide analogues as potential antiviral agents.
      J. Med. Chem., 39: 3263-3268 (1996).
      


1445. Morfin, F., Snoeck, R., Andrei, G. & De Clercq, E.
      Phenotypic resistance of herpes simplex virus type 1 strains selected in vitro with antiviral compounds and combinations thereof.
      Antiviral Chem. Chemother., 7: 270-275 (1996).
      


1446. Balzarini, J., Wedgwood, O., Kruining, J., Pelemans, H., Heijtink, R., De Clercq, E. & McGuigan, C.
      Anti-HIV and anti-HBV activity and resistance profile of 2’,3’-dideoxy-3’-thiacytidine (3TC) and its arylphosphoramidate derivative Cf 1109.
      Biochem. Biophys. Res. Commun., 225: 363-369 (1996).
      


1447. Augustijns, P., Annaert, P., Adriaens, S., De Clercq, E. & Kinget, R.
      High speed HPLC determination of bis(pivaloyloxymethyl)-PMEA and its degradation products, mono(POM)-PMEA and PMEA.
      J. Liq. Chrom. & Rel. Technol., 19: 2271-2283 (1996).
      


1448. Schmit, J.-C., Ruiz, L., Clotet, B., Raventos, A., Tor, J., Leonard, J., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Resistance-related mutations in the HIV-1 protease gene of patients treated for 1 year with the protease inhibitor ritonavir (ABT-538).
      AIDS, 10: 995-999 (1996).
      


1449. De Clercq, E.
      Chemotherapy of human immunodeficiency virus (HIV) infection: anti-HIV agents tar­geted at early steps in the virus replicative cycle.
      Biomed. & Pharmacother., 50: 207-215 (1996).
      


1450. Gordon, Y.J., Naesens, L., De Clercq, E., Maudgal, P.C. and Veckeneer, M.
      Treatment of adenoviral conjunctivitis with topical cidofovir.
      Cornea, 15: 546 (1996).
      


1451. Schols, D. & De Clercq, E.
      Human immunodeficiency virus type 1 gp120 induces anergy in human peripheral blood lymphocytes by inducing interleukin-10 production.
      J. Virol., 70: 4953-4960 (1996).
      


1452. Balzarini, J., Pelemans, H., Aquaro, S., Perno, C.-F., Witvrouw, M., Schols, D., De Clercq, E. & Karlsson, A.
      Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodefi­ciency virus type 1 replication.
      Mol. Pharmacol., 50: 394-401 (1996).
      


1453. Hossain, N., Hendrix, C., Lescrinier, E., Van Aerschot, A., Busson, R., De Clercq, E. & Herdewijn, P.
      Homo-N-nucleosides: incorporation into oligonucleotides and antiviral activity.
      Bioorg. Med. Chem. Lett., 6: 1465-1468 (1996).
      


1454. Pérez-Pérez, M.-J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of 2-deoxy-1,5-anhydro-D-mannitol nucleosides contai­ning a pyrimidine base moiety.
      Bioorg. Med. Chem. Lett., 6: 1457-1460 (1996).
      


1455. Snoeck, R., Andrei, G. & De Clercq, E.
      Patterns of resistance and sensitivity to antiviral compounds of drug-resistant strains of human cy­tomegalovirus selected in vitro
      Eur. J. Clin. Microbiol. Infect. Dis., 15: 574-579 (1996).
      


1456. Gueiffier, A., Lhassani, M., Elhakmaoui, A., Snoeck, R., Andrei, G., Chavignon, O., Teulade, J.-C., Kerbal, A., Essassi, E.M., Debouzy, J.-C., Witvrouw, M., Blache, Y., Balzarini, J., De Clercq, E. & Chapat, J.-P.
      Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents.
      J. Med. Chem., 39: 2856-2859 (1996).
      


1457. Balzarini, J., Karlsson, A., Aquaro, S., Perno, C.-F., Cahard, D., Naesens, L., De Clercq, E. & McGuigan, C.
      Mechanism of anti-HIV action of masked alaninyl d4T-MP derivatives.
      Proc. Natl. Acad. Sci. USA, 93: 7295-7299 (1996).
      


1458. Locher, C.P., Witvrouw, M., de Béthune, M.-P., Burch, M.T., Mower, H.F., Davis, H., Lasure, A., Pauwels, R., De Clercq, E. & Vlietinck, A.J.
      Antiviral activity of Hawaiian medicinal plants against human immunodeficiency virus type-1 (HIV-1).
      J. Phytomedicine, 2: 259-264 (1996).
      


1459. De Clercq, E.
      What can be expected from non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the treatment of human immunodeficiency virus type 1 (HIV-1) infections ?
      Rev. Med. Virol., 6: 97-117 (1996).
      


1460. McGuigan, C., Salgado, A., Yarnold, C., Harries, T.Y., De Clercq, E. & Balzarini, J.
      Novel nucleoside phosphoramidates as inhibitors of HIV: studies on the stereochemical requirements of the phosphoramidate amino acid.
      Antiviral Chem. Chemother., 7: 184-188 (1996).
      


1461. Van hemel, J., Esmans, E.L., De Groot, A., Dommisse, R.A., Balzarini, J.M. & De Clercq, E.
      Synthesis and biological evaluation of some acyclic pyridine C-nucleosides. Part two.
      Nucleosides & Nucleotides, 15: 1203-1221 (1996).
      


1462. Cobo, J., Melguizo, M., Sánchez, A., Nogueras, M. & De Clercq, E.
      A new method for the synthesis of 2-glycosylamino pyridines.
      Tetrahedron, 52: 5845-5856 (1996).
      


1463. De Clercq, E.
      Chemotherapy of viral infections.
      In: "Medical Microbiology", 4th ed., S. Baron (ed.). The University of Texas Medical Branch at Galveston, Texas, pp. 663-671 (1996).
      


1464. McGuigan, C., Cahard, D., Sheeka, H.M., De Clercq, E. & Balzarini, J.
      Phosphoramidate derivatives of d4T with improved anti-HIV efficacy retain full activity in thymidine kinase-deficient cells.
      Bioorg. Med. Chem. Lett., 6: 1183-1186 (1996).
      


1465. Kodama, E., Shigeta, S., Suzuki, T. & De Clercq, E.
      Application of a gastric cancer cell line (MKN-28) for anti-adenovirus screening using the MTT method.
      Antiviral Res., 31: 159-164 (1996).
      


1466. Shuto, S., Obara, T., Saito, Y., Andrei, G., Snoeck, R., De Clercq, E. & Matsuda, A.
      New neplanocin analogues 6. Synthesis and antiviral activity of 6'-homoneplanocin A.
      J. Med. Chem., 39: 2392-2399 (1996).
      


1467. McGuigan, C., Cahard, D., Sheeka, H.M., De Clercq, E. & Balzarini, J.
      Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue cul­ture and may act by the generation of a novel intracellular metabolite.
      J. Med. Chem., 39: 1748-1753 (1996).
      


1468. Leydet, A., El Hachemi, H., Boyer, B., Lamaty, G., Roque, J.P., Schols, D., Snoeck, R., Andrei, G., Ikeda, S., Neyts, J., Reymen, D., Esté, J., Witvrouw, M. & De Clercq, E.
      Polyanion inhibitors of human immunodeficiency virus and other viruses. Part 2. Poly­merized anionic surfactants derived from amino acids and dipeptides.
      J. Med. Chem., 39: 1626-1634 (1996).
      


1469. De Clercq, E.
      Therapeutic potential of cidofovir (HPMPC, VistideTM) for the treatment of DNA virus (i.e. herpes-, papova-, pox- and adenovirus) infections.
      Verh. K. Acad. Geneesk. Belg., 58: 19-49 (1996).
      


1470. Neyts, J., Meerbach, A., Mc Kenna, P. & De Clercq, E.
      Use of the yellow fever virus vaccine strain 17D for the study of strategies for the treat­ment of yellow fever virus infections.
      Antiviral Res., 30: 125-132 (1996).
      


1471. Bellarosa, D., Antonelli, G., Bambacioni, F., Giannotti, D., Viti, G., Nannicini, R., Gia­chetti, A., Dianzani, F., Witvrouw, M., Pauwels, R., Desmyter, J. & De Clercq, E.
      New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase.
      Antiviral Res., 30: 109-124 (1996).
      


1472. Leydet, A., Barthélémy, P., Boyer, B., Lamaty, G., Roque, J.-P., Witvrouw, M. & De Clercq, E.
      Polyanions inhibitors of human immunodeficiency virus. Part IV. - Polymerized anionic surfactants: influence of the density and distribution of anionic groups on the antiviral activity.
      Bioorg. Med. Chem. Lett., 6: 397-402 (1996).
      


1473. Balzarini, J., Brouwer, W.G., Dao, D.C., Osika, E.M. & De Clercq, E.
      Identification of novel thiocarboxanilide derivatives that suppress a variety of drug-resistant mutant human immunodeficiency virus type 1 strains at a potency similar to that for wild-type virus.
      Antimicrob. Agents Chemother., 40: 1454-1466 (1996).
      


1474. Herdewijn, P. & De Clercq, E.
      Classical antiviral agents and design of new antiviral agents (Section 16).
      In: "A Textbook of Drug Design and Development", P. Krogsgaard-Larsen, T. Liljefors and U. Madsen (eds.). Harwood Academic Publishers, London, United Kingdom, pp. 425-459 (1996).
      


1475. Groziak, M.P., Lin, R., Stevens, W.C., Wotring, L.L., Townsend, L.B., Balzarini, J., Witvrouw, M. & De Clercq, E.
      Definitive solution structures for the 6-formylated versions of 1-(ß-D-ribofuranosyl)-, 1-(2'-deoxy-ß-D-ribofuranosyl)-, and 1-ß-D-arabinofuranosyluracil, and of thymidine.
      Nucleosides & Nucleotides, 15: 1041-1057 (1996).
      


1476. Balzarini, J., Pelemans, H., Pérez-Pérez, M.-J., San-Félix, A., Camarasa, M.-J., De Clercq, E. & Karlsson, A.
      Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1, when combined with (-)2',3'-dideoxy-3'-thia­cytidine (3TC).
      Mol. Pharmacol., 49: 882-890 (1996).
      


1477. Jashés, M., González, M., López-Lastra, M., De Clercq, E. & Sandino, A.
      Inhibitors of infectious pancreatic necrosis virus (IPNV) replication.
      Antiviral Res., 29: 309-312 (1996).
      


1478. Esté, J.A., De Vreese, K., Witvrouw, M., Schmit, J.-C., Vandamme, A.-M., Anné, J., Desmyter, J., Henson, G.W., Bridger, G. & De Clercq, E.
      Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type 1.
      Antiviral Res., 29: 297-307 (1996).
      


1479. De Vreese, K., Reymen, D., Griffin, P., Steinkasserer, A., Werner, G., Bridger, G.J., Esté, J., James, W., Henson, G.W., Desmyter, J., Anné, J. & De Clercq, E.
      The bicyclams, a new class of potent human immunodeficiency virus inhibitors, block viral entry after binding.
      Antiviral Res., 29: 209-219 (1996).
      


1480. Vandevelde, M., Witvrouw, M., Schmit, J.C., Sprecher, S., De Clercq, E. & Tassignon, J.-P.
      ADA, a potential anti-HIV drug. Letter to the Editor.
      AIDS Res. Human Retrovir., 12: 567-568 (1996).
      


1481. Hiebl, J., Zbiral, E., von Janta-Lipinski, M., Balzarini, J. & De Clercq, E.
      Side-chain derivatives of biologically active nucleosides. Part 2. Synthesis and anti-HIV activity of 5'-C-methyl derivatives of 3'-fluoro-3'-deoxythymidine.
      Antiviral Chem. Chemother., 7: 173-177 (1996).
      


1482. Reymen, D., Witvrouw, M., Esté, J.A., Neyts, J., Schols, D., Andrei, G., Snoeck, R., Cushman, M., Hejchman, E. & De Clercq, E.
      Mechanism of the antiviral activity of new aurintricarboxylic acid analogues.
      Antiviral Chem. Chemother., 7: 142-152 (1996).
      


1483. Soler, F., Poujade, C., Evers, M., Carry, J.-C., Hénin, Y., Bousseau, A., Huet, T., Pau­wels, R., De Clercq, E., Mayaux, J.-F., Le Pecq, J.-B. & Dereu, N.
      Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry.
      J. Med. Chem., 39: 1069-1083 (1996).
      


1484. Kuipers, M.E., Huisman, J.G., Swart, P.J., de Béthune, M.-P., Pauwels, R., Schuitemaker, H., De Clercq, E. & Meijer, D.K.F.
      Mechanism of anti-HIV activity of negatively charged albumins: biomolecular interac­tion with the HIV-1 envelope protein gp120.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 11: 419-429 (1996).
      


1485. Mikhailov, S.N., Blaton, N., Rozenski, J., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Use of cyclohexene epoxides in the preparation of carbocyclic nucleosides.
      Nucleosides & Nucleotides, 15: 867-878 (1996).
      


1486. Evers, M., Poujade, C., Soler, F., Ribeill, Y., James, C., Lelièvre, Y., Gueguen, J.-C., Reisdorf, D., Morize, I., Pauwels, R., De Clercq, E., Hénin, Y., Bousseau, A., Mayaux, J.-F., Le Pecq, J.-B. & Dereu, N.
      Betulinic acid derivatives: a new class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action.
      J. Med. Chem., 39: 1056-1068 (1996).
      


1487. Balzarini, J., Aquaro, S., Perno, C.-F., Witvrouw, M., Holý, A. & De Clercq, E.
      Activity of the (R)-enantiomers of 9-(2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine against human immunodeficiency virus in different human cell systems.
      Biochem. Biophys. Res. Commun., 219: 337-341 (1996).
      


1488. Pauwels, R. & De Clercq, E.
      Development of vaginal microbicides for the prevention of heterosexual transmission of HIV.
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 11: 211-221 (1996).
      


1489. De Clercq, E.
      Non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of human immunodeficiency virus type 1 (HIV-1) infections: strategies to overcome drug resis­tance development.
      Med. Res. Rev., 16: 125-157 (1996).
      


1490. Kamps, J.A.A.M., Swart, P.J., Morselt, H.W.M., Pauwels, R., De Béthune, M.-P., De Clercq, E., Meijer, D.K.F. & Scherphof, G.L.
      Preparation and characterization of conjugates of (modified) human serum albumin and liposomes: drug carriers with an intrinsic anti-HIV activity.
      Biochim. Biophys. Acta, 1278: 183-190 (1996).
      


1491. Alvarez, R., San-Félix, A., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Novel TSAO derivatives. Synthesis and anti-HIV-1 activity of allofuranosyl-TSAO-T analogues.
      Nucleosides & Nucleotides, 15: 349-359 (1996).
      


1492. Verheggen, I., Van Aerschot, A., Rozenski, J., Janssen, G., De Clercq, E. & Herdewijn, P.
      Synthesis of 1,5-anhydrohexitol nucleosides as mimics of AZT, D4T and DDC.
      Nucleosides & Nucleotides, 15: 325-335 (1996).
      


1493. De Vreese, K., Kofler-Mongold, V., Leutgeb, C., Weber, V., Vermeire, K., Schacht, S., Anné, J., De Clercq, E., Datema, R. & Werner, G.
      The molecular target of bicyclams, potent inhibitors of human immunodeficiency virus replication.
      J. Virol., 70: 689-696 (1996).
      


1494. Bridger, G.J., Skerlj, R.T., Padmanabhan, S., Martellucci, S.A., Henson, G.W., Abrams, M.J., Joao, H.C., Witvrouw, M., De Vreese, K., Pauwels, R. & De Clercq, E.
      Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit human immunodeficiency virus replication. 2. Effect of heteroaromatic linkers on the activity of bicyclams.
      J. Med. Chem., 39: 109-119 (1996).
      


1495. Kuppermann, B.D., Assil, K.K., Vuong, C., Besen, G., Wiley, C.A., De Clercq, E., Bergeron-Lynn, G., Connor, J.D., Pursley, M., Munguia, D. & Freeman, W.R.
      Liposome-encapsulated (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine for long-acting therapy of viral retinitis.
      J. Infect. Dis.., 173: 18-23 (1996).
      


1496. Naesens, L., Balzarini, J., Bischofberger, N. & De Clercq, E.
      Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
      Antimicrob. Agents Chemother., 40: 22-28 (1996).
      


1497. McGuigan, C., Cahard, D., Salgado, A., De Clercq, E. & Balzarini, J.
      Phosphoramidates as potent prodrugs of anti-HIV nucleotides: studies in the amino region.
      Antiviral Chem. Chemother., 7: 31-36 (1996).
      


1498. Witvrouw, M., Seifert, J.-M., Henson, G.W., Martellucci, S.A., Desmyter, J. & De Clercq, E.
      Pharmacokinetics of the anti-HIV bicyclam SID791 (JM3100) in rabbits, as determined by both analytical and bioassay methods.
      Antiviral Chem. Chemother., 7: 27-30 (1996).
      



102 publications in the year 1995



1499. Meier, C., Habel, L.W., Balzarini, J. & De Clercq, E.
      5’,5’-Di-O-nucleosyl-O’-benzylphosphotriesters as potential prodrugs of 3’-azido-2’,3’-dideoxythymidine-5’-monophosphate.
      Liebigs Ann., 1995: 2203-2208 (1995).
      


1500. Meier, C., Habel, L.W., Balzarini, J. & De Clercq, E.
      Lipophilic -hydroxybenzylphosphonates as prodrugs of 3’-azido-2’,3’-dideoxythy­midine (AZT).
      Liebigs Ann., 1995: 2195-2202 (1995).
      


1501. De Hauwere, B., Lutz, A., Maudgal, P.C., Neyts, J. & De Clercq, E.
      An ocular model of adenovirus type 5 infection in the rabbit.
      Bull. Soc. belge Ophtalmol., 259: 33-42 (1995).
      


1502. Maruyama, T., Utsumi, K., Tomioka, H., Kasamoto, M., Sato, Y., Anné, J. & De Clercq, E.
      Synthesis, antiviral, antibacterial and antitumor cell activities of 2'-deoxy-2'-fluoropuro­mycin.
      Chem. Pharm. Bull., 43: 955-959 (1995).
      


1503. Snoeck, R. & De Clercq, E.
      Herpesvirus infections in immunocompromised patients.
      In: "Infectious Complications of Cancer", J. Klastersky (ed.). Kluwer Academic Publi­shers, Boston, Dordrecht, London, pp. 149-171 (1995).
      


1504. Neyts, J., Andrei, G., Balzarini, J., Snoeck, R. & De Clercq, E.
      Specific phosphorylation of 2-amino-7-[(1,3-dihydroxy-2-propoxymethyl)]purine (S2242) in human cytomegalovirus-infected human embryonic lung fibroblasts.
      Scand. J. Infect. Dis., 99, Suppl.: 115-116 (1995).
      


1505. Esteban, A.I., Juanes, O., Conde, S., Goya, P., De Clercq, E. & Martínez, A.
      New 1,2,6-thiadiazine dioxide acyclonucleosides: synthesis and antiviral evaluation.
      Bioorg. Med. Chem., 13: 1527-1535 (1995).
      


1506. Lewis, M., McMurry, T.B.H. & De Clercq, E.
      Fluorinated carbaacyclonucleosides: synthesis and evaluation of antiviral activity.
      Nucleosides & Nucleotides, 14: 1913-1927 (1995).
      


1507. Balzarini, J., Navé, J.-F., Becker, M.A., Tatibana, M. & De Clercq, E.
      Kinetic properties of adenine nucleotide analogues against purified 5-phosphoribosyl-1-pyrophosphate synthetases from E.coli, rat liver and human erythrocytes.
      Nucleosides & Nucleotides, 14: 1861-1871 (1995).
      


1508. Himpens, B., Proot, P., Neyts, J., De Smedt, H., De Clercq, E. & Casteels, R.
      Human cytomegalovirus modulates the Ca2+ response to vasopressin and ATP in human fibroblast cultures.
      Cell Calcium, 18: 111-119 (1995).
      


1509. Naesens, L., Balzarini, J. & De Clercq, E.
      The potential of acyclic nucleoside phosphonates as broad-spectrum antiviral agents.
      Advances in Biochemistry (Postepy Biochemii), 41 (Suppl.): 347-351 (1995).
      


1510. De Clercq, E.
      Chemotherapy of human immunodeficiency virus (HIV) infection based on chemothera­peutic intervention with early steps of the virus replicative cycle.
      Advances in Biochemistry (Postepy Biochemii), 41 (Suppl.): 338-342 (1995).
      


1511. De Clercq, E. & Balzarini, J.
      Knocking out human immunodeficiency virus through non-nucleoside reverse transcrip­tase inhibitors used as single agents or in combinations: a paradigm for the cure of AIDS ?
      Il Farmaco, 50: 735-747 (1995).
      


1512. Esté, J.A., Witvrouw, M., Tu, J., Desmyter, J., De Clercq, E. & Vandamme, A.-M.
      Inhibition of HIV type 1 tat-mediated trans-activation by oncostatin M in HLtat cells.
      AIDS Res. Human Retrovir, 11: 1355-1358 (1995).
      


1513. Ojwang, J.O., Buckheit, R.W., Pommier, Y., Mazumder, A., De Vreese, K., Esté, J.A., Reymen, D., Pallansch, L.A., Lackman-Smith, C., Wallace, T.L., De Clercq, E., McGrath, M.S. & Rando, R.F.
      T30177, an oligonucleotide stabilized by an intramolecular guanosine octet, is a potent inhibitor of laboratory strains and clinical isolates of human immunodeficiency virus type 1.
      Antimicrob. Agents Chemother., 39: 2426-2435 (1995).
      


1514. Pauwels, R., de Béthune, M.-P., Andries, K., Stoffels, P., Janssen, P. & De Clercq, E.
      Discovery, development and characterization of agents active against the AIDS virus.
      J. Receptor & Signal Transduction Res., 15: 609-616 (1995).
      


1515. Reymen, D., Naesens, L., Balzarini, J., Holý, A., Dvoraková, H. & De Clercq, E.
      Antiviral activity of selected acyclic nucleoside analogues against human herpesvirus type 6.
      Antiviral Res., 28: 343-357 (1995).
      


1516. Loakes, D., Brown, D.M., Mahmood, N., Balzarini, J. & De Clercq, E.
      Antiviral activity of bicyclic pyrimidine nucleosides.
      Antiviral Chem. Chemother., 6: 371-378 (1995).
      


1517. Ingate, S.T., Camarasa, M.-J., De Clercq, E. & Balzarini, J.
      Synthesis and anti-HIV-1 activity of [1-[2',5'-bis-O-(tert-butyldimethylsilyl)-ß-L-ribofu­ranosyl]thymine]-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-dioxide) (L-TSAO-T), the L-enantiomer of the highly specific HIV-1 reverse transcriptase inhibitor TSAO-T.
      Antiviral Chem. Chemother., 6: 365-370 (1995).
      


1518. Cheraghali, A.M., Kumar, R., Morin, K.W., De Clercq, E., Knaus, E.E. & Wiebe, L.I.
      A comparative study of 5-ethyl-2'-deoxyuridine and selected lipophilic 5,6-dihydro double/triple prodrugs.
      Antiviral Chem. Chemother., 6: 356-364 (1995).
      


1519. Acedo, M., De Clercq, E. & Eritja, R.
      Synthesis and biophysical and biological properties of oligonucleotides containing 2-aza-2'-deoxyinosine.
      J. Org. Chem., 60: 6262-6269 (1995).
      


1520. Balzarini, J., Andrei, G., Kumar, R., Knaus, E.E., Wiebe, L.I. & De Clercq, E.
      The cytostatic activity of 5-(1-azidovinyl)-2'-deoxyuridine (AzVDU) against herpes simplex virus thymidine kinase gene-transfected FM3A cells is due to inhibition of thymidylate synthase and enhanced by UV light ( = 254 nm) exposure.
      FEBS Lett., 373: 41-44 (1995).
      


1521. Joao, H.C., De Vreese, K., Pauwels, R., De Clercq, E., Henson, G.W. & Bridger, G.J.
      Quantitative structural activity relationship study of bis-tetraazaacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors.
      J. Med. Chem., 38: 3865-3873 (1995).
      


1522. Snoeck, R., Van Ranst, M., Andrei, G., De Clercq, E., De Wit, S., Poncin, M. & Clumeck, N.
      Treatment of anogenital papillomavirus infections with an acyclic nucleoside phos­phonate analogue.
      New Engl. J. Med., 333: 943-944 (1995).
      


1523. De Clercq, E.
      Trends in the development of new antiviral agents for the chemotherapy of infections caused by herpesviruses and retro­viruses.
      Rev. Med. Virol., 5: 149-164 (1995).
      


1524. Neyts, J., Reymen, D., Letourneur, D., Jozefonvicz, J., Schols, D., Este, J., Andrei, G., McKenna, P., Witvrouw, M., Ikeda, S., Clement, J. & De Clercq, E.
      Differential antiviral activity of derivatized dextrans.
      Biochem. Pharmacol., 50: 743-751 (1995).
      


1525. Wutzler, P., De Clercq, E., Wutke, K. & Färber, I.
      Oral brivudin vs. intravenous acyclovir in the treatment of herpes zoster in immunocom­promised patients: a randomized double-blind trial.
      J. Med. Virol., 46: 252-257 (1995).
      
      Neyts, J. & De Clercq, E.
      Effect of polyanionic compounds on intracutaneous and intravagi­nal herpesvirus infec­tion in mice: impact on the search for vaginal microbicides with anti-HIV activity
      J. Acquir. Immune Defic. Syndr. Human Retrovirol., 10: 8-12 (1995).
      


1526. Golankiewicz, B., Januszczyk, P., Ikeda, S., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of benzyl-substituted imi­dazo[1,5-a]-1,3,5-triazine (5,8-diaza-7,9-dideazapurine) deriva­tives.
      J. Med. Chem., 38: 3558-3565 (1995).
      


1527. Kundu, N.G., Mahanty, J.S., Spears, C.P., Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Palladium-catalyzed synthesis of (E)-5-(2-acylvinyl)-2'-deoxyuridines and their antiviral and cytotoxic activities.
      Bioorg. Med. Chem. Lett., 5: 1627-1632 (1995).
      


1528. Tanaka, H., Takashima, H., Ubasawa, M., Sekiya, K., Inouye, N., Baba, M., Shigeta, S., Walker, R.T., De Clercq, E. & Miyasaka, T.
      Synthesis and antiviral activity of 6-benzyl analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents.
      J. Med. Chem., 38: 2860-2865 (1995).
      


1529. Andrei, G., Snoeck, R. & De Clercq, E.
      Susceptibilities of several drug-resistant herpes simplex virus type 1 strains to alternative antiviral compounds.
      Antimicrob. Agents Chemother., 39: 1632-1635 (1995).
      


1530. Balzarini, J., Morin, K.W., Knaus, E.E., Wiebe, L.I. & De Clercq, E.
      Novel (E)-5-(2-iodovinyl)-2'-deoxyuridine derivatives as potential cytostatic agents against herpes simplex virus thymidine kinase gene transfected tumors.
      Gene Therapy, 2: 317-322 (1995).
      


1531. Harmsen, M.C., Swart, P.J., de Béthune, M.-P., Pauwels, R., De Clercq, E., The, T.H. & Meijer, D.K.F.
      Antiviral effects of plasma and milk proteins: lactoferrin shows potent activity against both human immunodeficiency virus and human cytomegalovirus replication in vitro.
      J. Infect. Dis., 172: 380-388 (1995).
      


1532. Tatebayashi, M., Neyts, J., Besen, G., Flores-Aguilar, M., Smith, I.L., Wiley, C.A., Spector, S.A., Bergeron-Lynn, G., Maudgal, P.C., De Clercq, E., Gangan, P.A., Chavez, E., Russack, V. & Freeman, W.R.
      Absence of infectious retinitis after injection of human cytomegalovirus into rabbit eyes.
      J. Infect. Dis., 171: 782-787 (1995).
      


1533. Pérez-Pérez, M.-J., Balzarini, J., Rozenski, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of phosphonate derivatives of enantiomeric dihydro-2H-pyranyl nucleosides.
      Bioorg. Med. Chem. Lett., 5: 1115-1118 (1995).
      


1534. Ingate, S., Pérez-Pérez, M.-J., De Clercq, E., Balzarini, J. & Camarasa, M.-J.
      Synthesis and anti-HIV-1 activity of novel TSAO-T derivatives modified at the 2'- and 5'-positions of the sugar moiety.
      Antiviral Res., 27: 281-299 (1995).
      


1535. Balzarini, J., Brouwer, W.G., Felauer, E.E., De Clercq, E. & Karlsson, A.
      Activity of various thiocarboxanilide derivatives against wild-type and several mutant human immunodeficiency virus type 1 strains.
      Antiviral Res., 27: 219-236 (1995).
      


1536. Balzarini, J., Weeger, M., Camarasa, M.-J., De Clercq, E. & Überla, K.
      Sensitivity/resistance profile of a simian immunodeficiency virus (SIV) containing the reverse transcriptase gene of human immunodeficiency virus type 1 (HIV-1) toward the HIV-1-specific non-nucleoside reverse transcriptase inhibitors.
      Biochem. Biophys. Res. Commun., 211: 850-856 (1995).
      


1537. Luyten, I., Jie, L., Van Aerschot, A., Pannecouque, C., Wigerinck, P., Rozenski, J., Hen­drix, C., Wang, C., Wiebe, L., Balzarini, J., De Clercq, E. & Herdewijn, P.
      2'-Deoxyuridines with a 5-heteroaromatic substituent: synthesis and biological evalua­tion.
      Antiviral Chem. Chemother., 6: 262-270 (1995).
      


1538. Balzarini, J., Pérez-Pérez, M.-J., Vélazquez, S., San-Félix, A., Camarasa, M.-J., De Clercq, E. & Karlsson, A.
      Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives).
      Proc. Natl. Acad. Sci. USA, 92: 5470-5474 (1995).
      


1539. De Clercq, E.
      Toward improved anti-HIV chemotherapy: therapeutic strategies for intervention with HIV infections.
      J. Med. Chem., 38: 2491-2517 (1995).
      


1540. Leydet, A., Barthélémy, Ph., Boyer, B., Lamaty, G., Roque, J.P., Bousseau, A., Evers, M., Hénin, Y., Snoeck, R., Andrei, G., Ikeda, S., Reymen, D. & De Clercq, E.
      Polyanion inhibitors of human immunodeficiency virus and other viruses. Part I - poly­merized anionic surfactants.
      J. Med. Chem., 38: 2433-2440 (1995).
      


1541. Neyts, J., Verbiest, A., Meerbach, A. & De Clercq, E.
      Human cytomegalovirus stimulates thymidylate synthase in human embryonic lung cells: a possible target for anti-HCMV therapy ?
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 1153-1156 (1995).
      


1542. Tusek-Bozic, Lj., Curic, M., Balzarini, J. & De Clercq, E.
      Biological activity of some dialkyl -anilinobenzylphosphonates and their palladium(II) complexes.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 777-781 (1995).
      


1543. Naesens, L., Neyts, J., Balzarini, J., Bischofberger, N. & De Clercq, E.
      In vivo antiretroviral efficacy of oral Bis(POM)-PMEA, the bis(pivaloyloxy-methyl)prodrug of 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 767-770 (1995).
      


1544. Meier, C., Habel, L., Laux, W., De Clercq, E. & Balzarini, J.
      Homo dinucleoside--hydroxyphosphonate diesters as prodrugs of the antiviral nucleo­side analogues 2',3'-dideoxythymidine and 3'-azido-2',3'-dideoxythymidine.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 759-762 (1995).
      


1545. Pérez-Pérez, M.-J., Doboszewski, B., De Clercq, E. & Herdewijn, P.
      Phosphonates derivatives of 2',3'-dideoxy-2',3'-didehydro-pentopyranosyl nucleosides.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 707-710 (1995).
      


1546. Hatse, S., Balzarini, J. & De Clercq, E.
      Induction of erythroid differentiation of human leukemia K-562 cells by the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 649-652 (1995).
      


1547. Girardet, J.-L., Gosselin, G., Périgaud, C., Balzarini, J., De Clercq, E. & Imbach, J.-L.
      Synthesis and antitumor properties of some neutral triesters of 5-fluoro-2'-deoxyuridine-5'-monophosphate and 3',5'-cyclic monophosphate.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 645-647 (1995).
      


1548. Jonckheere, H., Taymans, J.-M., Balzarini, J., Velázquez, S., Camarasa, M.-J., Desmyter, J., De Clercq, E. & Anné, J.
      Evidence for the involvement of the small subunit of HIV-1 reverse transcriptase (RT) in the TSAO-resistance.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 599-602 (1995).
      


1549. San-Félix, A., Alvarez, R., Velázquez, S., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Synthesis and anti-HIV-1 activity of 4- and 5-substituted 1,2,3-triazole-TSAO deriva­tives.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 595-598 (1995).
      


1550. Camarasa, M.J., Pérez-Pérez, M.J., Velázquez, S., San-Félix, A., Alvarez, R., Ingate, S., Jimeno, J.L., Karlsson, A., De Clercq, E. & Balzarini, J.
      TSAO derivatives: highly specific inhibitors of human immunodeficiency virus type-1 (HIV-1) replication.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 585-594 (1995).
      


1551. Baba, M., Tanaka, H., Miyasaka, T., Yuasa, S., Ubasawa, M., Walker, R.T. & De Clercq, E.
      HEPT derivatives: 6-benzyl-1-ethoxymethyl-5-isopropyluracil (MKC-442).
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 575-583 (1995).
      


1552. Reymen, D., Naesens, L., Balzarini, J., Holý, A. & De Clercq, E.
      Antiviral activity of selected nucleoside analogues against human herpes virus type 6.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 567-570 (1995).
      


1553. Andrei, G., Snoeck, R., Balzarini, J. & De Clercq, E.
      Combination of azidothymidine (AZT) and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) inhibits the replication of herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) and varicella zoster virus (VZV) strains that are deficient in the expression of the viral thymidine kinase (TK).
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 559-562 (1995).
      


1554. Gueffier, A., Blache, Y., Chapat, J.P., Elhakmaoui, A., Essassi, E.M., Andrei, G., Snoeck, R., De Clercq, E., Chavignon, O., Teulade, J.C. & Fauvelle, F.
      Synthesis and antiviral activity of 2- and 3-substituted imidazo[1,2-a]pyrimidine.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 551-554 (1995).
      


1555. Serafinowski, P., Dorland, E., Balzarini, J. & De Clercq, E.
      The synthesis and antiviral activity of some new S-adenosyl-L-homocysteine derivatives and their nucleoside precursors.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 545-547 (1995).
      


1556. Pannecouque, C., Van Poppel, K., Balzarini, J., Claes, P., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral evaluation of 3'-substituted thymidine analogues derived from 3'-amino-3'-deoxythymidine.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 541-544 (1995).
      


1557. Kalinichenko, E.N., Rubinova, E.B., Borisov, E.V., Balzarini, J., De Clercq, E. & Mikhailopulo, I.A.
      Stereospecific synthesis and anti-HIV activity of (Z)2'- and (E)3'-deoxy-2'(3')-C-(chloromethylene)pyrimidine nucleosides.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 533-536 (1995).
      


1558. Liu, J., Van Aerschot, A., Luyten, I., Wigerinck, P., Pannecouque, C., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activities of some new 5-heteroaromatic substituted derivatives of 2'-deoxyuridine.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 525-528 (1995).
      


1559. Santana, L., Teijeira, M., Uriarte, E., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of 1,2-carbonucleosides.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leuven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 521-523 (1995).
      


1560. Poopeiko, N.E., Poznanski, J., Drabikowska, A., Balzarini, J., De Clercq, E., Mik­hailopulo, I.A., Shugar, D. & Kulikowski, T.
      Synthesis, solution conformation and biological properties of 2',3'-dideoxy-3'-fluoro-D-erythro-pentofuranosides of 2-thiouracil and 2-thiothymine.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leu­ven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 435-437 (1995).
      


1561. Lazrek, H.B., Redwane, N., Rochdi, A., Barascut, J.L., Imbach, J.-L. & De Clercq, E.
      Synthesis of acycloalkenyl derivatives of pyrimidines and purines.
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leu­ven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 353-356 (1995).
      


1562. Ingate, S., San-Félix, A., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Synthesis of [1-[2',5'-bis-O-(t-butyldimethylsilyl)-ß-L-ribofuranosyl]thymine]-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-dioxide) (L-TSAO-T).
      Proceedings of the 11th International Round Table on Nucleosides and Nucleotides, Leu­ven, Belgium, 7-11 September 1994.
      Nucleosides & Nucleotides, 14: 299-301 (1995).
      


1563. Besen, G., Flores-Aguilar, M., Assil, K.K., Kupperman, B.D., Gangan, P., Pursley, M., Munguia, D., Vuong, C., De Clercq, E., Bergeron-Lynn, G., Azen, S.P. & Freeman, W.R.
      Long-term therapy of herpes retinitis in an animal model with high-concentrated liposome-encapsulated HPMPC.
      Arch. Ophthalmol., 113: 661-668 (1995).
      


1564. Dimmock, J.R., Pandeya, S.N., Quail, J.W., Pugazhenthi, U., Allen, T.M., Kao, G.Y., Balzarini, J. & De Clercq, E.
      Evaluation of the semicarbazones, thiosemicarbazones and bis-carbohydrazones of some aryl alicyclic ketones for anticonvulsant and other biological properties.
      Eur. J. Med. Chem., 30: 303-314 (1995).
      


1565. De Clercq, E.
      Antiviral therapy for human immunodeficiency virus infections.
      Clin. Microbiol. Rev., 8: 200-239 (1995).
      


1566. De Clercq, E. & Desmyter, J.
      EC Centralized facility and concerted action on design, synthesis, evaluation and deve­lopment of new antiviral compounds against AIDS.
      In "AIDS Research at EC Level", Biomedical and Health Research Vol. 6, A.-E. Baert, M.A. Koch, L. Montagnier, M.C. Razquin & D. Tyrrell (eds.).
      IOS Press, Amsterdam, The Netherlands, pp. 149-165 (1995).
      


1567. Thormar, H., Balzarini, J., Debyser, Z., Witvrouw, M., Desmyter, J. & De Clercq, E.
      Inhibition of visna virus replication and cytopathic effect in sheep choroid plexus cell cultures by selected anti-HIV agents.
      Antiviral Res., 27: 49-57 (1995).
      


1568. Baba, M., Balzarini, J., Pauwels, R. & De Clercq, E.
      HIV-1-specific reverse transcriptase inhibitors.
      In: "Anti-AIDS Drug Development. Challenges, Strategies and Prospects", P. Mohan & M. Baba (eds.). Harwood Academic Publi­shers, Chur, Switzerland, pp. 239-267 (1995).
      


1569. De Clercq, E.
      From anti-HIV agents to anti-AIDS chemotherapy: a critical ap­praisal.
      In: "Anti-AIDS Drug Development. Challenges, Strategies and Prospects", P. Mohan & M. Baba (eds.). Harwood Academic Publi­shers, Chur, Switzerland, pp. 1-37 (1995).
      


1570. Thormar, H., Georgsson, G., Pálsson, P.A., Balzarini, J., Naesens, L., Torsteinsdóttir, S. & De Clercq, E.
      Inhibitory effect of 9-(2-phosphonylmethoxyethyl)adenine on visna virus infection in lambs: a model for in vivo testing of candidate anti-human immunodeficiency virus drugs.
      Proc. Natl. Acad. Sci. USA, 92: 3283-3287 (1995).
      


1571. Balzarini, J., Baba, M. & De Clercq, E.
      Differential activity of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives against different human immunode­ficiency virus type 1 mutant strains.
      Antimicrob. Agents Chemother., 39: 998-1002 (1995).
      


1572. Dimmock, J.R., Kumar, P., Quail, J.W., Pugazhenthi, U., Yang, J., Chen, M., Reid, R.S., Allen, T.M., Kao, G.Y., Cole, S.P.C., Batist, G., Balzarini, J. & De Clercq, E.
      Synthesis and cytotoxic evaluation of some styryl ketones and related compounds.
      Eur. J. Med. Chem., 30: 209-217 (1995).
      


1573. Andrei, G., Snoeck, R., Reymen, D., Liesnard, C., Goubau, P., Desmyter, J. & De Clercq, E.
      Comparative activity of selected antiviral compounds against clinical isolates of varicella-zoster virus.
      Eur. J. Clin. Microbiol. Infect. Dis., 14: 318-328 (1995).
      


1574. Kirsch, L.S., Arevalo, J.F., Chavez de la Paz, E., Munguia, D., De Clercq, E. & Freeman, W.R.
      Intravitreal cidofovir (HPMPC) treatment of cytomegalovirus retinitis in patients with acquired immune deficiency syndrome.
      Ophthalmology, 102: 533-543 (1995).
      


1575. Kirsch, L.S., Arevalo, J.F., De Clercq, E., Chavez de la Paz, E., Munguia, D., Garcia, R. & Freeman, W.R.
      Phase I/II study of intravitreal cidofovir for the treatment of cytomegalovirus retinitis in patients with the acquired immunodeficiency syndrome.
      Am. J. Ophthalmol., 119: 466-476 (1995).
      


1576. De Clercq, E.
      Antiviral chemotherapy: where do we stand and what can we expect?
      Int. Antiviral News, 3: 52-54 (1995).
      


1577. Vahlenkamp, T.W., De Ronde, A., Balzarini, J., Naesens, L., De Clercq, E., van Eijk, M.J.T., Horzinek, M.C. & Egberink, H.F.
      (R)-9-(2-Phosphonylmethoxypropyl)-2,6-diaminopurine is a potent inhibitor of feline immunodeficiency virus infection.
      Antimicrob. Agents Chemother., 39: 746-749 (1995).
      


1578. Pannecouque, C., Busson, R., Balzarini, J., Claes, P., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral evaluation of 3'-substituted thymidine analogues derived from 3'-amino-3'-deoxythymidine.
      Tetrahedron, 51: 5369-5380 (1995).
      


1579. Cushman, M., Wang, P., Reymen, D., Este, J., Witvrouw, M., Neyts, J. & De Clercq, E.
      Anti-HIV and anti-HCMV activities of new aurintricarboxylic acid analogues.
      Antiviral Chem. Chemother., 6: 179-186 (1995).
      


1580. Balzarini, J., Jonckheere, H., Harrison, W.A., Dao, D.C., Anné, J., De Clercq, E. & Karlsson, A.
      Oxathiin carboxanilide derivatives: a class of non-nucleoside HIV-1-specific reverse transcriptase inhibitors (NNRTIs) that are active against mutant HIV-1 strains resistant to other NNRTIs.
      Antiviral Chem. Chemother., 6: 169-178 (1995).
      


1581. Velázquez, S., Alvarez, R., San-Félix, A., Jimeno, M.L., De Clercq, E., Balzarini, J. & Camarasa, M.J.
      Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase.
      J. Med. Chem., 38: 1641-1649 (1995).
      


1582. Siddiqi, S.M., Chen, X., Rao, J., Schneller, S.W., Ikeda, S., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      3-Deaza- and 7-deaza-5'-noraristeromycin and their antiviral properties.
      J. Med. Chem., 38: 1035-1038 (1995).
      


1583. Balzarini, J., Verstuyf, A., Hatse, S., Goebels, J., Sobis, H., Vandeputte, M. & De Clercq, E.
      The human immunodeficiency virus (HIV) inhibitor 9-(2-phosphonylmethoxyethyl)ade-nine (PMEA) is a strong inducer of differentiation of several tumor cell lines.
      Int. J. Cancer, 61: 130-137 (1995).
      


1584. Verheggen, I., Van Aerschot, A., Van Meervelt, L., Rozenski, J., Wiebe, L., Snoeck, R., Andrei, G., Balzarini, J., Claes, P., De Clercq, E. & Herdewijn, P.
      Synthesis, biological evaluation, and structure analysis of a series of new 1,5-anhydro­hexitol nucleosides.
      J. Med. Chem., 38: 826-835 (1995).
      


1585. Ho, W., Kukla, M.J., Breslin, H.J., Ludovici, D.W., Grous, P.P., Diamond, C.J., Miranda, M., Rodgers, J.D., Ho, C.Y., De Clercq, E., Pauwels, R., Andries, K., Janssen, M.A.C. & Janssen, P.A.J.
      Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. 4.
      J. Med. Chem., 38: 794-802 (1995).
      


1586. Breslin, H.J., Kukla, M.J., Ludovici, D.W., Mohrbacher, R., Ho, W., Miranda, M., Rodgers, J.D., Hitchens, T.K., Leo, G., Gauthier, D.A., Ho, C.Y., Scott, M.K., De Clercq, E., Pauwels, R., Andries, K., Janssen, M.A.C. & Janssen, P.A.J.
      Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo-[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives. 3.
      J. Med. Chem., 38: 771-793 (1995).
      


1587. Vandamme, A.-M., Van Dooren, S., Kok, W., Goubau, P., Fransen, K., Kievits, T., Schmit, J.-C., De Clercq, E. & Desmyter, J.
      Detection of HIV-1 RNA in plasma and serum samples using the NASBA amplification system compared to RNA-PCR.
      J. Virol. Methods, 52: 121-132 (1995).
      


1588. Van Cutsem, E., Snoeck, R., Van Ranst, M., Fiten, P., Opdenakker, G., Geboes, K., Jans­sens, J., Rutgeerts, P., Vantrappen, G. & De Clercq, E.
      Successful treatment of a squamous papilloma of the hypopharynx-esophagus by local injections of (S)-1-(3-hydroxy-2-phosphonyl­methoxypropyl)cytosine (HPMPC).
      J. Med. Virol., 45: 230-235 (1995).
      


1589. Hammerschmidt, F., Polsterer, J.-P., Zbiral, E., Balzarini, J. & De Clercq, E.
      Ein einfacher Weg zu 3'-Desoxy--L- und 3'-Desoxy-ß-D-apionucleosiden.
      Liebigs Ann., 1995: 559-565 (1995).
      


1590. Hammerschmidt, F., Öhler, E., Polsterer, J.-P., Zbiral, E., Balzarini, J. & De Clercq, E.
      Ein einfacher Weg zu D-Apio-ß-D-furanosyl- und 2'-Desoxyapio-ß-D-furanosylnucleo­siden.
      Liebigs Ann., 1995: 551-558 (1995).
      


1591. Johnson, C.R., Bhumralkar, D.R. & De Clercq, E.
      3'-C-trifluoromethyl ribonucleosides.
      Nucleosides & Nucleotides, 14: 185-194 (1995).
      


1592. Cushman, M., Golebiewski, W.M., Pommier, Y.G., Mazumder, A., Reymen, D., De Clercq, E., Graham, L. & Rice, W.G.
      Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and inte­grase.
      J. Med. Chem., 38: 443-452 (1995).
      


1593. Bridger, G.J., Skerlj, R.T., Thornton, D., Padmanabhan, S., Martellucci, S.A., Henson, G.W., Abrams, M.J., Yamamoto, N., De Vreese, K., Pauwels, R. & De Clercq, E.
      Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that in­hibit HIV replication. Effects of macrocyclic ring size and sub­stituents on the aromatic linker.
      J. Med. Chem., 38: 366-378 (1995).
      


1594. Balzarini, J. & De Clercq, E.
      Acyclic purine nucleoside phosphonates as retrovirus inhibitors.
      In: "Antiviral Chemotherapy", D.J. Jeffries & E. De Clercq (eds.). John Wiley & Sons, Chichester, Sussex, pp. 41-79 (1995).
      


1595. Jeffries, D. & De Clercq, E.
      Introduction.
      In: "Antiviral Chemotherapy", D.J. Jeffries & E. De Clercq (eds.). John Wiley & Sons, Chichester, Sussex, pp. xi-xxiii (1995)
      


1596. Manfredini, S., Baraldi, P.G., Bazzanini, R., Marangoni, M., Simoni, D., Balzarini, J. & De Clercq, E.
      Synthesis and cytotoxic activity of 6-vinyl- and 6-ethynyluridine and 8-vinyl- and 8-ethynyladenosine.
      J. Med. Chem., 38: 199-203 (1995).
      


1597. Neyts, J., Jähne, G., Andrei, G., Snoeck, R., Winkler, I. & De Clercq, E.
      In vivo antiherpesvirus activity of N-7-substituted acyclic nucleoside analog 2-amino-7-[(1,3-dihydroxy-2-propoxy)methyl]purine.
      Antimicrob. Agents Chemother., 39: 56-60 (1995).
      


1598. Bridger, G.J., Datema, R. & De Clercq, E.
      Bicyclams: potent and highly selective inhibitors of HIV-1 and HIV-2 replication.
      Int. Antiviral News, 3: 20-22 (1995).
      


1599. Calogeropoulou, I., Koufaki, M., Tsotinis, A., Balzarini, J., De Clercq, E. & Makriyannis, A.
      Synthesis and anti-HIV evaluation of alkyl and alkoxyethyl phosphodiester AZT deriva­tives
      Antiviral Chem. Chemother., 6: 43-49 (1995).
      


1600. Loakes, D., Brown, D.M., Mahmood, N., Balzarini, J. & De Clercq, E.
      Antiviral activity of N4-aminocytidine derivatives related to AZT.
      Antiviral Chem. Chemother., 6: 9-16 (1995).
      



76 publications in the year 1994



1601. Kaminsky, R., Zweygarth, E. & De Clercq, E.
      Antitrypanosomal activity of phosphonylmethoxyalkyl purines.
      J. Parasitol., 80: 1026-1030 (1994).
      


1602. Neyts, J. & De Clercq, E.
      New inhibitors of cytomegalovirus replication: in vitro evaluation, mechanism of action, and in vivo activity.
      Verh. K. Acad. Geneesk. Belg., 56: 561-592 (1994).
      


1603. Balzarini, J. & De Clercq, E.
      Biochemical pharmacology of nucleoside analogues active against HIV.
      In: "Textbook of AIDS Medicine", S. Broder, T.C. Merigan & D. Bolognesi (eds.). Wil­liams & Wilkins, Baltimore, Maryland, pp. 751-772 (1994).
      


1604. Kolokouris, N., Ikeda, S. & De Clercq, E.
      3-Cyclopentyl-1-adamantanamines and adamantanemethanamines. Antiviral activity evaluation and convulsions studies.
      Il Farmaco, 49: 641-647 (1994).
      


1605. Van hemel, J., Esmans, E.L., Alderweireldt, F.C., Dommisse, R.A., De Groot, A., Balza­rini, J. & De Clercq, E.
      Synthesis and biological evaluation of some acyclic pyridine C-nucleosides. Part one.
      Nucleosides & Nucleotides, 13: 2345-2366 (1994).
      


1606. De Clercq, E.
      Resistance of human immunodeficiency virus type 1 (HIV-1) to non-nucleoside HIV-1-specific reverse transcriptase inhibitors.
      Proceedings of the 11th Future Trends in Chemotherapy/Interdisciplinary World Con­gress on Antimicrobial and Anticancer Drugs, Palexpo, Geneva, Switzerland, 25-27 April 1994. Bioscience Ediprint Inc., Carouge-Geneva.
      Int. J. Immunotherapy, 10: 145-158 (1994).
      


1607. Alvarez, R., Velázquez, S., San-Félix, A., Aquaro, S., De Clercq, E., Perno, C.-F., Karlsson, A., Balzarini, J. & Camarasa, M.J.
      1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-ß-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
      J. Med. Chem., 37: 4185-4194 (1994).
      


1608. Pauwels, R., Andries, K., Debyser, Z., Kukla, M.J., Schols, D., Breslin, H.J., Woesten­borghs, R., Desmyter, J., Janssen, M.A.C., De Clercq, E. & Janssen, P.A.J.
      New tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of human immunodeficiency virus type 1 replication and are syner­gistic with 2',3'-dideoxynucleoside analogs.
      Antimicrob. Agents Chemother., 38: 2863-2870 (1994).
      


1609. Neyts, J., Andrei, G., Snoeck, R., Jähne, G., Winkler, I., Helsberg, M., Balzarini, J. & De Clercq, E.
      The N-7-substituted acyclic nucleoside analog 2-amino-7-[(1,3-dihydroxy-2-pro­poxy)methyl]purine is a potent and selective inhibitor of herpesvirus replication.
      Antimicrob. Agents Chemother., 38: 2710-2716 (1994).
      


1610. Balzarini, J., Karlsson, A., Meichsner, C., Paessens, A., Riess, G., De Clercq, E. & Kleim, J.-P.
      Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to qui­noxaline S-2720.
      J. Virol., 68: 7986-7992 (1994).
      


1611. Swartling, D., Fry, M., Morgan, M., Biehl, E., Balzarini, J. & De Clercq, E.
      The synthesis, fluorescence and antiviral studies of 3'-amino-2',3'-dide­oxythymidine/substituted 10-cyano-9-isothiocyanatoan­thracene adducts.
      Nucleosides & Nucleotides, 13: 2013-2019 (1994).
      


1612. Tronchet, J.M.J., Zsély, M., Capek, K., Komaromi, I., Geoffroy, M., De Clercq, E. & Balzarini, J.
      Anti-HIV derivatives of 1-(2,3-dideoxy-3-N-hydroxyamino-ß-D-threo-pentofurano­syl)thymine.
      Nucleosides & Nucleotides, 13: 1871-1889 (1994).
      


1613. Heijtink, R.A, Kruining, J., de Wilde, G.A., Balzarini, J., De Clercq, E. & Schalm, S.W.
      Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture.
      Antimicrob. Agents Chemother, 38: 2180-2182 (1994).
      


1614. De Clercq, E.
      How to overcome resistance of HIV-1 to HIV-1-specific reverse transcriptase inhibitors ? (Letter)
      AIDS, 8: 1020-1021 (1994).
      


1615. Wnuk, S.F., Yuan, C.-S., Borchardt, R.T., Balzarini, J., De Clercq, E. & Robins, M.J.
      Nucleic acid related compounds. 84. Synthesis of 6'(E and Z)-halohomovinyl derivatives of adenosine, inactivation of S-adenosyl-L-homocysteine hydrolase, and correlation of anticancer and antiviral potencies with enzyme inhibition.
      J. Med. Chem., 37: 3579-3587 (1994).
      


1616. Balzarini, J., Kruining, J., Heijtink, R. & De Clercq, E.
      Comparative anti-retrovirus and anti-hepadnavirus activity of three different classes of nucleoside phosphonate derivatives.
      Antiviral Chem. Chemother., 5: 360-365 (1994).
      


1617. Witvrouw, M., Desmyter, J. & De Clercq, E.
      Antiviral portrait series: 4. Polysulfates as inhibitors of HIV and other enveloped viruses.
      Antiviral Chem. Chemother., 5: 345-359 (1994).
      


1618. Melguizo, M., Sánchez, A., Nogueras, M., Low, J.N., Howie, R.A., Andrei, G. & De Clercq, E.
      Facile preparation of 9-H-pyrimido[4,5-b][1,4]diazepine deriva­tives from 4,5-diamino­pyrimidines and ethyl pyruvate.
      Tetrahedron, 50: 13511-13522 (1994).
      


1619. Naesens, L., Balzarini, J. & De Clercq, E.
      Therapeutic potential of PMEA as an antiviral drug.
      Rev. Med. Virol., 4: 147-159 (1994).
      


1620. Jonckheere, H., Taymans, J.-M., Balzarini, J., Velázquez, S., Camarasa, M.-J., Desmyter, J., De Clercq, E. & Anné, J.
      Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-dioxide)] (TSAO) derivatives is determined by the mutation Glu138  Lys on the p51 subunit.
      J. Biol. Chem., 269: 25255-25258 (1994).
      


1621. Ikeda, S., Neyts, J. & De Clercq, E.
      Host defense mechanisms against murine cytomegalovirus infection induced by poly I:C in severe combined immune deficient (SCID) mice.
      Proc. Soc. Exp. Biol. Med., 207: 191-196 (1994).
      


1622. Damonte, E., Neyts, J., Pujol, C.A., Snoeck, R., Andrei, G., Ikeda, S., Witvrouw, M., Reymen, D., Haines, H., Matulewicz, M.C., Cerezo, A., Coto, C.E. & De Clercq, E.
      Antiviral activity of a sulfated polysaccharide from the red seaweed Nothogenia fasti­giata.
      Biochem. Pharmacol., 47: 2187-2192 (1994).
      


1623. Golankiewicz, B., Ostrowski, T., Andrei, G., Snoeck, R. & De Clercq, E.
      Tricyclic analogues of acyclovir and ganciclovir. Influence of substituents in the hetero­cyclic moiety on the antiviral activity.
      J. Med. Chem., 37: 3187-3190 (1994).
      


1624. Elhakmaoui, A., Gueiffier, A., Milhavet, J.-C., Blache, Y., Chapat, J.-P., Chavignon, O., Teulade, J.-C., Snoeck, R., Andrei, G. & De Clercq, E.
      Synthesis and antiviral activity of 3-substituted imidazo[1,2-a]pyridines.
      Bioorg. Med. Chem. Lett., 4: 1937-1940 (1994).
      


1625. Dimmock, J.R., Arora, V.K., Quail, J.W., Pugazhenthi, U., Allen, T.M., Kao, G.Y. & De Clercq, E.
      Cytotoxic evaluation of some 3,5-diarylidene-4-piperidones and various related quater­nary ammonium compounds and analogs.
      J. Pharm. Sci., 83: 1124-1130 (1994).
      


1626. Kolocouris, N., Foscolos, G.B., Kolocouris, A., Marakos, P., Pouli, N., Fytas, G., Ikeda, S. & De Clercq, E.
      Synthesis and antiviral activity evaluation of some aminoadaman­tane derivatives.
      J. Med. Chem., 37: 2896-2902 (1994).
      


1627. Villani, N., Caliò, R., Balestra, E., Balzarini, J., De Clercq, E., Fabrizi, E., Perno, C.-F. & Del Gobbo, V.
      9-(2-Phosphonylmethoxyethyl)adenine increases the survival of influenza virus-infected mice by enhancement of the immune system.
      Antiviral Res., 25: 81-89 (1994).
      


1628. Todoulou, O.G., Papadaki-Valiraki, A.E., Ikeda, S. & De Clercq, E.
      Synthesis and antiviral activity of some new 1H-1,2,4-triazole derivatives.
      Eur. J. Med. Chem., 29: 611-620 (1994).
      


1629. Manfredini, S., Baraldi, P.G., Bazzanini, R., Guarneri, M., Simoni, D., Balzarini, J. & De Clercq, E.
      Geiparvarin analogues. 4. Synthesis and cytostatic activity of geiparvarin analogues bearing a carbamate moiety or a furocoumarin fragment on the alkenyl side chain.
      J. Med. Chem., 37: 2401-2405 (1994).
      


1630. Ding, L., Grehn, L., De Clercq, E., Andrei, G., Snoeck, R., Balzarini, J., Fransson, B. & Ragnarsson, U.
      Synthesis and antiviral activity of three pyrazole analogues of distamycin A.
      Acta Chem. Scand., 48: 498-505 (1994).
      


1631. Balzarini, J., Kleim, J.-P., Riess, G., Camarasa, M.-J., De Clercq, E. & Karlsson, A.
      Sensitivity of (138 Glu  Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors.
      Biochem. Biophys. Res. Commun., 201: 1305-1312 (1994).
      


1632. Keizer, H.J., De Bruijn, E.A., Tjaden, U.R. & De Clercq, E.
      Inhibition of fluorouracil catabolism in cancer patients by the antiviral agent (E)-5-(2-bromovinyl)-2'-deoxyuridine.
      J. Cancer Res. Clin. Oncol., 120: 545-549 (1994).
      


1633. De Clercq, E.
      New developments in the chemotherapy of lentivirus (human immunodeficiency virus) infections: sensitivity/resistance of HIV-1 to non-nucleoside HIV-1-specific inhibitors.
      Proceedings of the New York Academy of Sciences Conference on "Slow Infections of the Central Nervous System: the Legacy of Dr. Björn Sigurdsson, Reykjavik, Iceland, 2-5 June 1993.
      Ann. N.Y. Acad. Sci., 724: 438-456 (1994).
      


1634. Van Aerschot, A., Zhigang, N., Rozenski, J., Claes, P., De Clercq, E. & Herdewijn, P.
      2-Hydroxyethoxyethylated bases as acyclic analogues of 1,5-anhydrohexitol nucleoside derivatives.
      Nucleosides & Nucleotides, 13: 1791-1800 (1994).
      


1635. Balzarini, J., Karlsson, A., Sardana, V.V., Emini, E.A., Camarasa, M.-J. & De Clercq, E.
      Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant HIV-1(E138K)RT HIV-1 mutants or select for highly resistant (Y181C  C181I)RT HIV-1 mutants.
      Proc. Natl. Acad. Sci. USA, 91: 6599-6603 (1994).
      


1636. Snoeck, R., Andrei, G., Balzarini, J., Reymen, D. & De Clercq, E.
      Dipyridamole potentiates the activity of various acyclic nucleoside phosphonates against varicella-zoster virus, herpes simplex virus and human cytomegalovirus.
      Antiviral Chem. Chemother., 5: 312-321 (1994).
      


1637. Witvrouw, M., Este, J.A., Mateu, M.Q., Reymen, D., Andrei, G., Snoeck, R., Ikeda, S., Pauwels, R., Bianchini, N.V., Desmyter, J. & De Clercq, E.
      Activity of a sulfated polysaccharide extracted from the red seaweed Aghardhiella tenera against human immunodeficiency virus and other enveloped viruses.
      Antiviral Chem. Chemother., 5: 297-303 (1994).
      


1638. De Clercq, E.
      Antiviral activity spectrum and target of action of different classes of nucleoside ana­logues.
      Nucleosides & Nucleotides, 13: 1271-1295 (1994).
      


1639. Balzarini, J., Bohman, C., Walker, R.T. & De Clercq, E.
      Comparative cytostatic activity of different antiherpetic drugs against herpes simplex virus thymidine kinase gene-transfected tumor cells.
      Mol. Pharmacol., 45: 1253-1258 (1994).
      


1640. Andrei, G., Snoeck, R. & De Clercq, E.
      Human brain tumour cell lines as cell substrate to demonstrate sensitivity/resistance of herpes simplex virus types 1 and 2 to nucleoside analogues.
      Antiviral Chem. Chemother., 5: 263-270 (1994).
      


1641. Gosselin, G., Périgaud, C., Bergogne, M.-C., Balzarini, J., De Clercq, E. & Imbach, J.-L.
      Synthesis and biological evaluation of new 5,6-dichlorobenzimidazole nucleoside de­rivatives.
      Antiviral Chem. Chemother., 5: 243-256 (1994).
      


1642. Snoeck, R., Andrei, G. & De Clercq, E.
      Chemotherapy of varicella zoster virus infections.
      Int. J. Antimicrob. Chemother., 4: 211-226 (1994).
      


1643. Flores-Aguilar, M., Huang, J.-S., Wiley, C.A., De Clercq, E., Vuong, C., Bergeron-Lynn, G., Chandler, B., Munguia, D. & Freeman, W.R.
      Long-acting treatment of viral retinitis with (S)-1-(3-hydroxy-2-phosphonylmethoxypro­pyl)cytosine.
      J. Infect. Dis., 169: 642-647 (1994).
      


1644. Todoulou, O.G., Papadaki-Valiraki, A.E., Filippatos, E.C., Ikeda, S. & De Clercq, E.
      Synthesis and anti-myxovirus activity of some novel N,N'-disubstituted thioureas.
      Eur. J. Med. Chem., 29: 127-131 (1994).
      


1645. Bruning, J.H., Persoons, M., Lemström, K., Stals, F.S., De Clercq, E. & Bruggeman, C.A.
      Enhancement of transplantation-associated atherosclerosis by CMV, which can be pre­vented by antiviral therapy in the form of HPMPC.
      Transplant Int., 7, Suppl. 1: S365-S370 (1994).
      


1646. De Clercq, E.
      Trends in drug development for the treatment of AIDS. Compounds interfering with the initial stages of the HIV replicative cycle.
      Proceedings of the 2nd European Congress of Pharmaceutical Sciences, Berlin, Germany, September 29-October 1, 1994.
      Eur. J. Pharm. Sci., 2: 4-6 (1994).
      


1647. De Clercq, E.
      Human immunodeficiency virus (HIV) inhibitors targeted at the reverse transcriptase.
      In: "Proceedings of the Third European Conference of the Medicinal Chemistry Group of the Atlantic Arc", Cardiff, Wales, United Kingdom, 3-5 July 1994. Smith, H.J., Nicholls, P.J. & Le Baut, G. (Eds.). Library Graphic Services, University of Wales, Cardiff, United Kingdom, pp. 1-12 (1994).
      


1648. Balzarini, J. & De Clercq, E.
      Role of antiherpetic drugs in the chemotherapy of herpes simplex virus thymidine kinase gene-transfected tumor cells.
      Int. Antiviral News, 2: 82-84 (1994).
      


1649. Siddiqi, S.M., Chen, X., Schneller, S.W., Ikeda, S., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      An epimer of 5'-noraristeromycin and its antiviral properties
      J. Med. Chem., 37: 1382-1384 (1994).
      


1650. Sági, G., Ötvös, L., Ikeda, S., Andrei, G., Snoeck, R. & De Clercq, E.
      Synthesis and antiviral activities of 8-alkynyl-, 8-alkenyl-, and 8-alkyl-2'-deoxyadenosine analogues.
      J. Med. Chem., 37: 1307-1311 (1994).
      


1651. Mayaux, J.F., Bousseau, A., Pauwels, R., Huet, T., Hénin, Y., Dereu, N., Evers, M., Soler, F., Poujade, C., De Clercq, E. & Le Pecq, J.B.
      Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.
      Proc. Natl. Acad. Sci. USA, 91: 3564-3568 (1994).
      


1652. De Clercq, E.
      In vitro detection of antiviral activity.
      Proceedings of the Symposium on "In Vitro and Ex Vivo Test Systems to Rationalize Drug Design and Delivery", Paris, France, 13-14 December 1993.
      In "Minutes Collection", Crommelin, D., Couvreur, P. & Duchêne, D. (Eds.). Editions de Santé, Paris, France, pp. 108-125 (1994).
      


1653. Verberckmoes, F., Esmans, E.L., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of some D-arabino- and D-lyxofuranosyl-pyridine C-nucleosides.
      Nucleosides & Nucleotides, 13: 511-525 (1994).
      


1654. Tanaka, H., Baba, M., Takahashi, E., Matsumoto, K., Kittaka, A., Walker, R.T., De Clercq, E. & Miyasaka, T.
      Design and synthesis of regioisomeric analogues of a specific anti-HIV-1 agent 1-[(2-hy­droxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).
      Nucleosides & Nucleotides, 13: 155-162 (1994).
      


1655. De Clercq, E., Vandamme, A.-M., Schols, D. & Debyser, Z.
      Potential chemotherapeutic targets in the replicative cycle of HIV.
      In "Design of Enzyme Inhibitors as Drugs. Vol. 2". Chapter 6 (Enzyme Targets as an Approach to Therapy for HIV Infections), M. Sandler & H.J. Smith (Eds.). Oxford Uni­versity Press, Oxford, pp. 192-225 (1994).
      


1656. Otake, T., Schols, D., Witvrouw, M., Naesens, L., Nakashima, H., Moriya, T., Kurita, H., Matsumoto, K., Ueba, N. & De Clercq, E.
      Modified cyclodextrin sulphates (mCDS11) have potent inhibitory activity against HIV and high oral bioavailability.
      Antiviral Chem. Chemother., 5: 155-161 (1994).
      


1657. Baba, M., Shigeta, S., Yuasa, S., Takashima, H., Sekiya, K., Ubasawa, M., Tanaka, H., Miyasaka, T., Walker, R.T. & De Clercq, E.
      Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro.
      Antimicrob. Agents Chemother., 38: 688-692 (1994).
      


1658. De Clercq, E., Yamamoto, N., Pauwels, R., Balzarini, J., Witvrouw, M., De Vreese, K., Debyser, Z., Rosenwirth, B., Peichl, P., Datema, R., Thornton, D., Skerlj, R., Gaul, F., Padmanabhan, S., Bridger, G., Henson, G. & Abrams, M.
      Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100.
      Antimicrob. Agents Chemother., 38: 668-674 (1994).
      


1659. Snoeck, R., Andrei, G., Gérard, M., Silverman, A., Hedderman, A., Balzarini, J., Sadzot-Delvaux, C., Tricot, G., Clumeck, N. & De Clercq, E.
      Successful treatment of progressive mucocutaneous infection due to acyclovir- and foscarnet-resistant herpes simplex virus with (S)-1-(3-hydroxy-2-phosphonyl­methoxypropyl)cytosine (HPMPC).
      Clin. Infect. Dis., 18: 570-578 (1994).
      


1660. Snoeck, R., Gérard, M., Sadzot-Delvaux, C., Andrei, G., Balzarini, J., Reymen, D., Ahadi, N., De Bruyn, J.M., Piette, J., Rentier, B., Clumeck, N. & De Clercq, E.
      Meningoradiculoneuritis due to acyclovir-resistant varicella zoster virus in an acquired immune deficiency syndrome patient.
      J. Med. Virol., 42: 338-347 (1994).
      


1661. Siddiqi, S.M., Chen, X., Schneller, S.W., Ikeda, S., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      Antiviral enantiomeric preference for 5'-noraristeromycin.
      J. Med. Chem., 37: 551-554 (1994).
      


1662. Bohman, C., Balzarini, J., Wigerinck, P., Van Aerschot, A., Herdewijn, P. & De Clercq, E.
      Mechanism of cytostatic action of novel 5-(thien-2-yl)- and 5-(furan-2-yl)-substituted pyrimidine nucleoside analogues against tumor cells transfected by the thymidine kinase gene of herpes simplex virus.
      J. Biol. Chem., 269: 8036-8043 (1994).
      


1663. De Clercq, E.
      Non-nucleoside reverse transcriptase inhibitors (NNRTIs).
      Exp. Opin. Invest. Drugs, 3: 253-271 (1994).
      


1664. Ikeda, S., Wong, M.F., Mohan, P. & De Clercq, E.
      Selective inhibition of myxovirus replication by a novel series of cholesterol-naphthale­nesulfonic acid hybrid molecules.
      Antiviral Chem. Chemother., 5: 122-127 (1994).
      


1665. Yokota, T., Konno, K., Shigeta, S., Holý, A., Balzarini, J. & De Clercq, E.
      Inhibitory effects of acyclic nucleoside phosphonate analogues on hepatitis B virus DNA synthesis in HB611 cells.
      Antiviral Chem. Chemother., 5: 57-63 (1994).
      


1666. San-Félix, A., Velázquez, S., Pérez-Pérez, M.J., Balzarini, J., De Clercq, E. & Camarasa, M.J.
      Novel series of TSAO-T derivatives. Synthesis and anti-HIV-1 activity of 4-, 5- and 6-substituted pyrimidine analogues.
      J. Med. Chem., 37: 453-460 (1994).
      


1667. Vandamme, A.-M., Debyser, Z., Pauwels, R., De Vreese, K., Goubau, P., Youle, M., Gazzard, B., Stoffels, P.A., Cauwenbergh, G.F., Anné, J., Andries, K., Janssen, P.A.J., Desmyter, J. & De Clercq, E.
      Characterization of HIV-1 strains isolated from patients treated with TIBO R82913.
      AIDS Res. Human Retrovir., 10: 39-46 (1994).
      


1668. Ikeda, S., Neyts, J., Verma, S., Wickramasinghe, A., Mohan, P. & De Clercq, E.
      In vitro and in vivo inhibition of ortho- and paramyxovirus infections by a new class of sulfonic acid polymers interacting with virus-cell binding and/or fusion.
      Antimicrob. Agents Chemother., 38: 256-259 (1994).
      


1669. Baba, M., Shigeta, S., Yuasa, S., Niwa, T., Yamamoto, M., Yabuuchi, S., Takashima, H., Ubasawa, M., Tanaka, H., Miyasaka, T., Walker, R.T., Balzarini, J. & De Clercq, E.
      Effect of human serum concentration on the in vitro anti-HIV-1 activity of HEPT deriva­tives: relation to their lipophilicity and serum protein binding.
      Proceedings of the Fourth Meeting of the Japanese Association of Antiviral Chemothe­rapy, Nagoya, Japan, 4-5 February 1993.
      In: "Progress of Antiviral Research in Japan", K. Ono (ed.). Japanese Association of Antiviral Chemotherapy, pp. 127-130 (1994).
      


1670. Yamamoto, N., Nakashima, H., Baba, M. & De Clercq, E.
      A novel class of bicyclam targeted at HIV uncoating (in Japanese).
      Proceedings of the Fourth Meeting of the Japanese Association of Antiviral Chemothe­rapy, Nagoya, Japan, 4-5 February 1993.
      In: "Progress of Antiviral Research in Japan", K. Ono (ed.). Japanese Association of Antiviral Chemotherapy, pp. 124-126 (1994).
      


1671. McGuigan, C., Pathirana, R.N., Davies, M.P.H., Balzarini, J. & De Clercq, E.
      Diaryl phosphate derivatives act as pro-drugs of AZT with reduced cytotoxicity com­pared to the parent nucleoside.
      Bioorg. Med. Chem. Lett., 4: 427-430 (1994).
      


1672. De Clercq, E.
      HIV resistance to reverse transcriptase inhibitors.
      Biochem. Pharmacol., 47: 155-169 (1994).
      


1673. Neyts, J. & De Clercq, E.
      Mechanism of action of acyclic nucleoside phosphonates against herpes virus replication.
      Biochem. Pharmacol., 47: 39-41 (1994).
      


1674. Ikeda, S., Nishiya, S., Yamamoto, A., Yamase, T., Nishimura, C. & De Clercq, E.
      Antiviral activity of a Keggin polyoxotungstate PM-19 against herpes simplex virus in mice.
      Antiviral Chem. Chemother., 5: 47-50 (1994).
      


1675. Hartmann, K., Balzarini, J., Higgins, J., De Clercq, E. & Pedersen, N.C.
      In vitro activity of acyclic nucleoside phosphonate derivatives against feline immunode­ficiency virus in Crandell feline kidney cells and feline peripheral blood lymphocytes.
      Antiviral Chem. Chemother., 5: 13-19 (1994).
      


1676. Caliò, R., Villani, N., Balestra, E., Sesa, F., Holý, A., Balzarini, J., De Clercq, E., Perno, C.F. & Del Gobbo, V.
      Enhancement of natural killer activity and interferon induction by different acyclic nucleoside phosphonates.
      Antiviral Res., 23: 77-89 (1994).
      



75 publications in the year 1993



1677. De Clercq, E.
      Strategies for the selective inhibition of human immunodeficiency virus replication.
      Proceedings of the International Symposium on Recent Advances in Chemotherapeutic Agents, Seoul, Korea, 19-20 August 1993.
      Research Center for New Drug Development, Seoul National University, Korea, pp. 69-86 (1993).
      


1678. Stals, F.S., Zeytinoglu, A., Havennith, M., De Clercq, E. & Bruggeman, C.A.
      Comparative effect of (S)-1-(3-hydroxy-2-phosphonylmethoxypro­pyl)cytosine and 9-(1,3-dihydroxy-2-propoxymethyl)guanine treat­ment on cytomegalovirus-induced inter­stitial pneumonitis in allogeneic bone marrow transplant recipient rats.
      Transplantation Proc., 25: 1248-1249 (1993).
      


1679. Perno, C.F., Del Gobbo, V., Balzarini, J., Balestra, E., Milanese, G., Aquaro, S., Sesa, F., Holý, A., De Clercq, E., Villani, N. & Caliò, R.
      Inhibition of HIV replication and enhancement of immune functions by the acyclic nucleoside phosphonate 9-(2-phosphonyl-methoxyethyl)adenine (PMEA).
      In "Combination Therapies 2", A.L. Goldstein & E. Garaci (eds.). Plenum Press, New York, pp. 115-122 (1993).
      


1680. Kukla, M.J., Breslin, H.J., De Clercq, E., Pauwels, R., Andries, K. & Janssen, P.A.J.
      Discovery and development of TIBO as a potential anti-AIDS therapeutic.
      Proceedings of the "First International Symposium on Recent Advances in the Chemistry of Anti-Infective Agents", Churchill College, Cambridge, United Kingdom, 5-8 July 1992.
      In "Recent Advances in the Chemistry of Anti-Infective Agents", P.H. Bentley & R. Ponsford (eds.), Royal Society of Chemistry (Industrial Division Fine Chemicals and Medicinals), pp. 266-281 (1993).
      


1681. De Clercq, E.
      Antiviral agents: characteristic activity spectrum depending on the molecular target they interact with.
      In "Advances in Virus Research", K. Maramorosch, F.A. Murphy & A.J. Shatkin (eds.), vol. 42, Academic Press, Orlando, Florida, pp. 1-55 (1993).
      


1682. De Clercq, E.
      Towards a "cure" for AIDS. Strategies for the selective inhibition of HIV replication.
      Proceedings of the Second F.T.I. (Flanders Technology Interna­tional) Conference, Nature, Ghent, Belgium, 3-6 May 1993. Flanders Technology International Foundation, Brussels, Belgium, pp. 1-22 (1993).
      


1683. Hosoya, M., Shigeta, S., Ishii, T., Suzuki, H. & De Clercq, E.
      Comparative inhibitory effects of various nucleoside and nonnucleoside analogues on replication of influenza virus types A and B in vitro and in ovo.
      J. Infect. Dis., 168: 641-646 (1993).
      


1684. Papadaki-Valiraki, A., Todoulou, O., Filippatos, E., Tsotinis, A., Ikeda, S. & De Clercq, E.
      Synthesis and antiviral activity of some new benzofuran derivatives.
      Arzneimittelforschung (Drug Research), 43: 1363-1366 (1993).
      


1685. Pérez-Pérez, M.-J., Balzarini, J., De Clercq, E. & Camarasa, M.-J.
      Glycosyl-oxycarbonylaminosulfonyl-2',3'-dideoxynucleoside derivatives as lipophilic nucleotide mimics. Synthesis and anti-HIV activity.
      Bioorg. & Med. Chem., 1: 279-284 (1993).
      


1686. Papadaki-Valiraki, A., Papakonstantinou-Garoufalias, S., Marakos, P., Chytyroglou-Lada, A., Hosoya, M., Ikeda, S., Balzarini, J. & De Clercq, E.
      Synthesis, antifungal, antibacterial and antiviral effects of some adamantaneketoxime ethers.
      Il Farmaco, 48: 1091-1102 (1993).
      


1687. Marquez, V.E., Lim, B.B., Driscoll, J.S., Snoeck, R., Balzarini, J., Ikeda, S., Andrei, G. & De Clercq, E.
      Cyclopentene carbocyclic nucleosides related to the antitumor nucleoside clitocine and their conversion to 8-aza-neplanocin analogues. Synthesis and antiviral activity.
      J. Heterocyclic Chem., 30: 1393-1398 (1993).
      


1688. De Vos, E., Esmans, E.L., Alderweireldt, F.C., Balzarini, J. & De Clercq, E.
      Synthesis of 2-carbamoylmethyl-6-ß-D-ribofuranosylpyridine with the aid of a Pd(O)-catalyzed reaction.
      J. Heterocyclic Chem., 30: 1245-1252 (1993).
      


1689. Jansen, R.W., Schols, D., Pauwels, R., De Clercq, E. & Meijer, D.K.F.
      Novel, negatively charged, human serum albumins display potent and selective in vitro anti-human immunodeficiency virus type 1 activity.
      Mol. Pharmacol., 44: 1003-1007 (1993).
      


1690. Chen, X., Schneller, S.W., Ikeda, S., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of 5'-deoxypyrazofurin.
      J. Med. Chem., 36: 3727-3730 (1993).
      


1691. Bârzu, T., Level, M., Petitou, M., Lormeau, J.-C., Choay, J., Schols, D., Baba, M., Pau­wels, R., Witvrouw, M. & De Clercq, E.
      Preparation and anti-HIV activity of O-acylated heparin and dermatan sulfate derivatives with low anticoagulant effect.
      J. Med. Chem., 36: 3546-3555 (1993).
      


1692. Velázquez, S., San-Félix, A., Pérez-Pérez, M.J., Balzarini, J., De Clercq, E. & Camarasa, M.J.
      TSAO analogues 3. Synthesis and anti-HIV-1 activity of 2',5'-bis-O-(tert-butyldi­methylsilyl)-ß-D-ribofuranosyl 3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-di­oxide)-purine and purine-modified nucleosides.
      J. Med. Chem., 36: 3230-3239 (1993).
      


1693. Snoeck, R., Gérard, M., Sadzot-Delvaux, C., Andrei, G., Balzarini, J., Reymen, D., Piette, J., Rentier, B., Clumeck, N. & De Clercq, E.
      Meningoradiculoneuritis due to acyclovir-resistant varicella-zoster virus in a patient with AIDS
      J. Infect. Dis., 168: 1330-1331 (1993).
      


1694. Balzarini, J., Karlsson, A., Wang, L., Bohman, C., Horská, K., Votruba, I., Fridland, A., Van Aerschot, A., Herdewijn, P. & De Clercq, E.
      EICAR (5-ethynyl-1-ß-D-ribofuranosylimidazole-4-carboxamide): a novel potent inhibi­tor of inosinate dehydrogenase activity and guanylate biosynthesis.
      J. Biol. Chem., 268: 24591-24598 (1993).
      


1695. Neyts, J. & De Clercq, E.
      Strategies for the treatment and prevention of cytomegalovirus infections.
      Int. J. Antimicrob. Agents, 3: 187-204 (1993).
      


1696. Neyts, J. & De Clercq, E.
      Efficacy of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine for the treatment of lethal vaccinia virus infections in severe combined immune deficiency (SCID) mice.
      J. Med. Virol., 41: 242-246 (1993).
      


1697. Ikeda, S., Nishiya, S., Yamamoto, A., Yamase, T., Nishimura, C. & De Clercq, E.
      Activity of the Keggin polyoxotungstate PM-19 against herpes simplex virus type 2 in­fection in immunosuppressed mice: role of peritoneal macrophage activation.
      J. Med. Virol., 41: 191-195 (1993).
      


1698. Thormar, H., Balzarini, J., Holý, A., Jindrich, J., Rosenberg, I., Debyser, Z., Desmyter, J. & De Clercq, E.
      Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogues.
      Antimicrob. Agents Chemother., 37: 2540-2544 (1993).
      


1699. Balzarini, J., Karlsson, A. & De Clercq, E.
      Human immunodeficiency virus type 1 drug-resistance patterns with different 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives.
      Mol. Pharmacol., 44: 694-701 (1993).
      


1700. Dvoráková, H., Holý, A., Masojídková, M., Votruba, I., Balzarini, J., Snoeck, R. & De Clercq, E.
      Synthesis and antiviral activity of acyclic nucleoside and nucleotide derivatives of 8-azaadenine.
      Proceedings of the IXth Symposium on the Chemistry of Nucleic Acids Components, Trest Castle, Czech Republic, 12-18 September 1993.
      Collect. Czech. Chem. Commun., 58: 253-255 (1993).
      


1701. Verheggen, I., Pillet, N., Van Aerschot, A., De Clercq, E. & Herdewijn, P.
      Synthesis and anti-herpesvirus activity of nucleosides with a 1,5-anhydrohexitol moiety.
      Proceedings of the IXth Symposium on the Chemistry of Nucleic Acids Components, Trest Castle, Czech Republic, 12-18 September 1993.
      Collect. Czech. Chem. Commun., 58: 64-67 (1993).
      


1702. Kulikowski, T., Poznanski, J., Balzarini, J., Van Aerschot, A. & De Clercq, E.
      Synthesis, conformation and anti-HIV activity of 3'-substituted 2',3'-dideoxy-5-hydroxy­methyluridines.
      Proceedings of the IXth Symposium on the Chemistry of Nucleic Acids Components, Trest Castle, Czech Republic, 12-18 September 1993.
      Collect. Czech. Chem. Commun., 58: 44-46 (1993).
      


1703. Tanaka, H., Baba, M., Yamamoto, T., Mori, S., Walker, R.T., De Clercq, E. & Miyasaka, T.
      Synthesis of a potential photoaffinity labelling reagent for HIV-1 reverse transcriptase.
      Bioorg. Med. Chem. Lett., 3: 1681-1686 (1993).
      


1704. Van Aerschot, A., Mamos, P., Weyns, N.J., Ikeda, S., De Clercq, E. & Herdewijn, P.
      Antiviral activity of C-alkylated purine nucleosides obtained by cross-coupling with tetraalkyltin reagents.
      J. Med. Chem., 36: 2938-2942 (1993).
      


1705. Lewis, M., McMurry, T.B.H. & De Clercq, E.
      9-(1-Fluoro-5-hydroxypentan-2-yl)-9H-guanine: synthesis and evaluation of antiviral ac­tivity
      J. Chem. Soc. Perkin Trans. 1, 1993: 2107-2110 (1993).
      


1706. Ikeda, S., Neyts, J., Yamamoto, N., Murrer, B., Theobald, B., Bossard, G., Henson, G., Abrams, M., Picker, D. & De Clercq, E.
      In vitro activity of a novel series of polyoxosilicotungstates against human myxo-, her­pes- and retroviruses.
      Antiviral Chem. Chemother., 4: 253-262 (1993).
      


1707. De Clercq, E.
      Anti-HIV agents interfering with the initial stages of the HIV replicative cycle.
      In "HIV Molecular Organization, Pathogenicity and Treatment", W.J.W. Morrow & N.L. Haigwood (Eds.), Elsevier Science Publishers B.V., pp. 267-292 (1993).
      


1708. Snoeck, R., Andrei, G., De Clercq, E., Gerard, M., Clumeck, N., Tricot, G. & Sadzot-Delvaux, C.
      A new topical treatment for resistant herpes simplex infections (Letter).
      New Engl. J. Med., 329: 968-969 (1993).
      


1709. Balzarini, J., Karlsson, A., Pérez-Pérez, M.-J., Camarasa, M.-J. & De Clercq, E.
      Knocking-out concentrations of HIV-1-specific inhibitors com­pletely suppress HIV-1 infection and prevent the emergence of drug-resistant virus.
      Virology, 196: 576-585 (1993).
      


1710. Balzarini, J., Karlsson, A., Pérez-Pérez, M.-J., Camarasa, M.-J., Tarpley, W.G. & De Clercq, E.
      Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combi­nations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy.
      J. Virol., 67: 5353-5359 (1993).
      


1711. De Clercq, E.
      Approaches to the antiviral treatment of HIV infection.
      In "The HIV Expert: A Comprehensive Review of HIV and its Management". The Well­come Foundation Ltd., Wellcome Group Marketing, Langley Court, Beckenham, pp. 5.1-5.10 (1993).
      


1712. Neyts, J., Stals, F., Atherton, S., Persoons, M., Bruggeman, C. & De Clercq, E.
      Efficacy of HPMPC in the treatment of CMV infections in various animal models.
      Proceedings of the 4th International CMV Conference on "Multi-Disciplinary Approach to Understanding Cytomegalovirus Disease", Institut Pasteur, Paris, France, 18-21 April 1993.
      In "Multidisciplinary Approach to Understanding Cytomegalovirus Disease", S. Michel­son and S.A. Plotkin (eds.). Elsevier Science Publisher, Amsterdam, pp. 279-285 (1993).
      


1713. Snoeck, R., Neyts, J. & De Clercq, E.
      Strategies for the treatment of cytomegalovirus infections.
      Proceedings of the 4th International CMV Conference on "Multi-Disciplinary Approach to Understanding Cytomegalovirus Disease", Institut Pasteur, Paris, France, 18-21 April 1993.
      In "Multidisciplinary Approach to Understanding Cytomegalovirus Disease", S. Michel­son and S.A. Plotkin (eds.). Elsevier Science Publisher, Amsterdam, pp. 269-278 (1993).
      


1714. Lagneaux, L., Delforge, A., Snoeck, R., De Clercq, E., Stryckmans, P. & Bron, D.
      Perturbation of cytokine production by bone marrow stromal cells after cytomegalovirus infection.
      Proceedings of the 4th International CMV Conference on "Multi-Disciplinary Approach to Understanding Cytomegalovirus Disease", Institut Pasteur, Paris, France, 18-21 April 1993.
      In "Multidisciplinary Approach to Understanding Cytomegalovirus Disease", S. Michel­son and S.A. Plotkin (eds.). Elsevier Science Publisher, Amsterdam, pp. 111-116 (1993).
      


1715. Andrei, G. & De Clercq, E.
      Molecular approaches for the treatment of hemorrhagic fever virus infections.
      Antiviral Res., 22: 45-75 (1993).
      


1716. De Clercq, E.
      Antivirals for the treatment of herpesvirus infections.
      J. Antimicrob. Chemother., 32, Suppl. A: 121-132 (1993).
      


1717. Balzarini, J., Naesens, L., Bohman, C., Pérez-Pérez, M.-J., San-Félix, A., Camarasa, M.-J. & De Clercq, E.
      Metabolism and pharmacokinetics of the anti-HIV-1-specific inhibitor [1-[2',5'-bis-O-(tert-butyldimethylsilyl)-ß-D-ribofuranosyl]-3-N-methyl-thymine]-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-dioxide) (TSAO-m3T).
      Biochem. Pharmacol., 46: 69-77 (1993).
      


1718. Ikeda, S., Neyts, J., Matsuura, M., Kiso, M., Hasegawa, A., Nishimura, C. & De Clercq, E.
      Protective activity of lipid A analogue GLA-60 against murine cytomegalovirus infection in mice.
      J. Med. Virol., 40: 222-227 (1993).
      


1719. Baba, M., Schols, D., Mohan, P., De Clercq, E. & Shigeta, S.
      Inhibition of HIV-1-induced cytopathogenicity, syncytium formation, and virus-cell binding by naphthalenedisulphonic acids through interaction with the viral envelope gp120 glycoprotein.
      Antiviral Chem. Chemother., 4: 229-234 (1993).
      


1720. Snoeck, R., Andrei, G., Neyts, J., Schols, D., Cools, M., Balzarini, J. & De Clercq, E.
      Inhibitory activity of S-adenosylhomocysteine hydrolase inhibitors against human cy­tomegalovirus replication.
      Antiviral Res., 21: 197-216 (1993).
      


1721. De Clercq, E.
      Therapeutic potential of HPMPC as an antiviral drug.
      Rev. Med. Virol., 3: 85-96 (1993).
      


1722. Ikeda, S., Neyts, J., Matsuura, M., Kiso, M., Hasegawa, A., Nishimura, C. & De Clercq, E.
      Protective activity of the lipid A analogue GLA-60 against murine cytomegalovirus in­fection in immunodeficient mice.
      J. Gen. Virol., 74: 1399-1403 (1993).
      


1723. Verheggen, I., Van Aerschot, A., Toppet, S., Snoeck, R., Janssen, G., Claes, P., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiherpes virus activity of 1,5-anhydrohexitol nucleosides.
      J. Med. Chem., 36: 2033-2040 (1993).
      


1724. Baba, M., Yuasa, S., Niwa, T., Yamamoto, M., Yabuuchi, S., Takashima, H., Ubasawa, M., Tanaka, H., Miyasaka, T., Walker, R.T., Balzarini, J., De Clercq, E. & Shigeta, S.
      Effect of human serum on the in vitro anti-HIV-1 activity of 1-[(2-hy­droxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) deriva­tives as related to their lipo­philicity and serum protein bin­ding.
      Biochem. Pharmacol., 45: 2507-2512 (1993).
      


1725. Neyts, J., Stals, F., Bruggeman, C. & De Clercq, E.
      Activity of the anti-HIV agent 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine against cytomegalovirus in vitro and in vivo.
      Eur. J. Clin. Microbiol. Infect. Dis., 12: 437-446 (1993).
      


1726. Balzarini, J., Pérez-Pérez, M.-J., San-Félix, A., Velázquez, S., Camarasa, M.-J., Van­damme, A.-M., Karlsson, A. & De Clercq, E.
      TSAO derivatives: a novel class of HIV-1-specific inhibitors.
      Proceedings of the "3rd International Symposium on the Chemical Synthesis of Antibio­tics and Related Microbial Products", Kloster Banz, Germany, 20-25 September 1992.
      In "Antibiotics and Antiviral Compounds. Chemical Synthesis and Modification", K. Krohn, H. Kirst & H. Maas (eds.). VCH Verlags­gesellschaft mbH, Weinheim, Germany, pp. 403-420 (1993).
      


1727. Balzarini, J., Karlsson, A., Vandamme, A.-M., Pérez-Pérez, M.-J., Vrang, L., Öberg, B., Bäckbro, K., Unge, T., San-Félix, A., Velazquez, S., Camarasa, M.-J. & De Clercq, E.
      Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxa­thiole-2",2"-dioxide)]-ß-D-pentofuranosyl (TSAO) nucleoside analogues retain sensiti­vity to HIV-1-specific nonnucleoside inhibitors.
      Proc. Natl. Acad. Sci. USA, 90: 6952-6956 (1993).
      


1728. Herdewijn, P., Balzarini, J. & De Clercq, E.
      2',3'-Dideoxynucleoside analogues as anti-HIV agents.
      In "Advances in Antiviral Drug Design", vol. 1, E. De Clercq (ed.). JAI Press Inc., Greenwich, Connecticut, pp. 233-318 (1993).
      


1729. Heijtink, R.A., de Wilde, G.A., Kruining, J., Berk, L., Holý, A., Balzarini, J., De Clercq, E. & Schalm, S.W.
      Antiviral activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) on human and duck hepatitis B virus infection.
      Antiviral Res., 21: 141-153 (1993).
      


1730. Siddiqi, S.M., Raissian, M., Schneller, S.W., Ikeda, S., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      (±)-7-deazaaristeromycin lacking the hydroxymethyl substituent.
      Bioorg. Med. Chem. Lett., 3: 663-666 (1993).
      


1731. Mikhailopulo, I.A., Zaitseva, G.V., Vaaks, E.V., Balzarini, J., De Clercq, E., Rosemeyer, H. & Seela, F.
      Synthesis of 2'-azido-2',3'-didehydro-2',3'-dideoxythymidine.
      Liebigs Ann. Chem., 1993: 513-519 (1993).
      


1732. McGuigan, C., Pathirana, R.N., Balzarini, J. & De Clercq, E.
      Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT.
      J. Med. Chem., 36: 1048-1052 (1993).
      


1733. de la Cruz, A., Elguero, J., Goya, P., Martinez, A. & De Clercq, E.
      Synthesis and biological evaluation of 4-quinolone ribosides.
      J. Chem. Soc. Perkin Trans. I, 845-849 (1993)
      


1734. Neyts, J., Sobis, H., Snoeck, R., Vandeputte, M. & De Clercq, E.
      Efficacy of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine and 9-(1,3-dihy­droxy-2-propoxymethyl)guanine in the treatment of intracerebral murine cytomegalovi­rus infections in immunocompe­tent and immunodeficient mice.
      Eur. J. Clin. Microbiol. Infect. Dis., 12: 269-279 (1993).
      


1735. De Clercq, E.
      Anti-HIV activity of sulfated polysaccharides.
      Proceedings of the ACS Polysaccharide Symposium, 204th National Meeting of the American Chemical Society, Washington DC, USA, 23-28 August 1992.
      In "Carbohydrates and Carbohydrate Polymers, Analysis, Biotech­nology, Modification, Antiviral, Biomedical and Other Applica­tions", M. Yalpani (ed.). ATL Press, Mt. Pros­pect, Illinois, pp. 87-100 (1993).
      


1736. Balzarini, J., Karlsson, A., Camarasa, M.-J. & De Clercq, E.
      HIV-1 strains selected for resistance against one particular class of HIV-1-specific reverse transcriptase inhibitors may retain sensitivity to other classes of HIV-1-specific inhibitors.
      Internat. Antiviral News, 1: 66-68 (1993).
      


1737. Debyser, Z., De Vreese, K., Knops-Gerrits, P.P., Baekelandt, V., Bhikhabhai, R., Strand­berg, B., Pauwels, R., Anné, J., Desmyter, J. & De Clercq, E.
      Kinetics of different human immunodeficiency virus type 1 reverse transcriptases resis­tant to human immunodeficiency virus type 1-specific reverse transcriptase inhibitors.
      Mol. Pharmacol., 43: 521-526 (1993).
      


1738. De Clercq, E.
      HIV-1-specific RT inhibitors: higly selective inhibitors of human immunodeficiency virus type 1 that are specifically targeted at the viral reverse transcriptase.
      Med. Res. Rev., 13: 229-258 (1993).
      


1739. Balzarini, J., Bohman, C. & De Clercq, E.
      Differential mechanism of cytostatic effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine, 9-(2,3-dihydroxy-2-propoxymethyl)-guanine, and other antiherpetic drugs on tumor cells transfected by the thymidine kinase gene of herpes simplex virus type 1 or type 2.
      J. Biol. Chem., 268: 6332-6337 (1993).
      


1740. De Clercq, E. & Snoeck, R.
      Inhibiteurs hautement spécifiques du virus de l'immunodéficience humaine de type I qui sont particulièrement ciblés au niveau de la transcriptase réverse.
      Path. Biol., 41: 230-236 (1993).
      


1741. Siddiqi, S.M., Schneller, S.W., Ikeda, S., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      S-Adenosyl-L-homocysteine hydrolase inhibitors as antiviral agents: 5'-deoxyaristero­mycin.
      Nucleosides & Nucleotides, 12: 185-198 (1993).
      


1742. Maruyama, T., Hanai, Y., Sato, Y., Snoeck, R., Andrei, G., Hosoya, M., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of carbocyclic oxetanocin analogues (C-OXT-A, C-OXT-G) and related compounds. II.
      Chem. Pharm. Bull., 41: 516-521 (1993).
      


1743. Wigerinck, P., Kerremans, L., Claes, P., Snoeck, R., Maudgal, P.C., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of 5-thien-2-yl-2'-deoxyuridine analogues.
      J. Med. Chem., 36: 538-543 (1993).
      


1744. Chen, X., Siddiqi, S.M., Schneller, S.W., Snoeck, R., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral properties of carbocyclic 3'-oxa-2',3'-dideoxyguanosine and its 7-deazaguanosine analogue.
      Antiviral Res., 20: 333-345 (1993).
      


1745. Balzarini, J., Velazquez, S., San-Felix, A., Karlsson, A., Perez-Perez, M.-J., Camarasa, M.-J. & De Clercq, E.
      Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-ß-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodefi­ciency virus type 1-specific non-nucleoside analogues.
      Mol. Pharmacol., 43: 109-114 (1993).
      


1746. Pauwels, R., Andries, K., Debyser, Z., Van Daele, P., Schols, D., Stoffels, P., De Vreese, K., Woestenborghs, R., Vandamme, A.-M., Janssen, C.G.M., Anné, J., Cauwenbergh, G., Desmyter, J., Heykants, J., Janssen, M.A.C., De Clercq, E. & Janssen, P.A.J.
      Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of -anilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase.
      Proc. Natl. Acad. Sci. USA, 90: 1711-1715 (1993).
      


1747. Naesens, L., Neyts, J., Balzarini, J., Holý, A., Rosenberg, I. & De Clercq, E.
      Efficacy of oral 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the treatment of retrovirus and cytomegalovirus infections in mice.
      J. Med. Virol., 39: 167-172 (1993).
      


1748. Balzarini, J., Holý, A., Jindrich, J., Naesens, L., Snoeck, R., Schols, D. & De Clercq, E.
      Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enan­tiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine.
      Antimicrob. Agents Chemother., 37: 332-338 (1993).
      


1749. Stals, F.S., Zeytinoglu, A., Havenith, M., De Clercq, E. & Bruggeman, C.A.
      Rat cytomegalovirus-induced pneumonitis after allogeneic bone marrow transplantation: effective treatment with (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine.
      Antimicrob. Agents Chemother., 37: 218-223 (1993).
      


1750. Villalón, M.D.G., Gil-Fernández, C. & De Clercq, E.
      Activity of several S-adenosylhomocysteine hydrolase inhibitors against African swine fever virus replication in Vero cells.
      Antiviral Res., 20: 131-144 (1993).
      


1751. Balzarini, J., Karlsson, A., Perez-Perez, M.-J., Vrang, L., Walbers, J., Zhang, H., Öberg, B., Vandamme, A.-M., Camarasa, M.-J. & De Clercq, E.
      HIV-1-Specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase.
      Virology, 192: 246-253 (1993).
      



78 publications in the year 1992



1752. De Clercq, E., Neyts, J., Naesens, L. & Balzarini, J.
      Therapeutic potential of acyclic nucleoside phosphonates in the treatment of herpes- and retrovirus infections (i.e. HPMPC against MCMV infection in SCID mice).
      Proceedings of Antiviral Drug Congress (The Fifth International Antiviral Symposium and the Second Korean-American AIDS Symposium), Seoul, Korea, 21-25 June 1992.
      Research Center for New Drug Development, Seoul National University, Korea, pp. 144-150 (1992).
      


1753. Fedorov, I.I., Krayevsky, A.A., Balzarini, J. & De Clercq E.
      Adducts of 3'-azido-2',3'-dideoxythymidine 5'-phosphate or 5'-hydrogenphosphonate as inhibitors of retroviral cytopathicity and cell transformation in culture.
      Molekulyarnaya Biologiya, 26: 1122-1127 (1992).
      Mol. Biol., 26: 749-752 (1992).
      


1754. Pauwels, R., Andries, K., Debyser, Z., Janssen, P.A.J., Kukla, M., Schols, D., Desmyter, J. & De Clercq, E.
      TIBO derivatives: a new class of highly potent and specific inhibitors of HIV-1 replica­tion.
      Biochem. Soc. Trans., 20: 509-512 (1992).
      


1755. De Clercq, E.
      La chimiothérapie du SIDA.
      La Recherche, 23: 288-295 (1992).
      


1756. Gordon, Y.J., Romanowski, E., Araullo-Cruz, T. & De Clercq, E.
      Pretreatment with topical 0.1% (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine inhibits adenovirus type 5 replication in the New Zealand rabbit ocular model.
      Cornea, 11: 529-533 (1992).
      


1757. Yamamoto, N., Schols, D., De Clercq, E., Debyser, Z., Pauwels, R., Balzarini, J., Naka­shima, H., Baba, M., Hosoya, M., Snoeck, R., Neyts, J., Andrei, G., Murrer, B.A., Theo­bald, B., Bossard, G., Henson, G., Abrams, M. & Picker, D.
      Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents.
      Mol. Pharmacol., 42: 1109-1117 (1992).
      


1758. Serafinowski, P., Dorland, E., Harrap, K.R., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of some new S-adenosyl-L-homo­cysteine derivatives.
      J. Med. Chem., 35: 4576-4583 (1992).
      


1759. Fedorov, I.I., Kazmina, E.M., Novicov, N.A., Gurskaya, G.V., Bochkarev, A.V., Jasko, M.V., Victorova, L.S., Kukhanova, M.K., Balzarini, J., De Clercq, E. & Krayevsky, A.
      3'-C-Branched 2'-deoxy-5-methyluridines: synthesis, enzyme inhi­bition, and antiviral properties
      J. Med. Chem., 35: 4567-4575 (1992).
      


1760. Snoeck, R., Andrei, G., Schols, D. & De Clercq, E.
      Activity of different antiviral drug combinations against human cytomegalovirus replica­tion in vitro.
      Eur. J. Clin. Microbiol. Infect. Dis., 11: 1144-1155 (1992).
      


1761. Cushman, M., Wang, P., Stowell, J.G., Schols, D. & De Clercq, E.
      Structural investigation and anti-HIV activities of high molecular weight ATA polymers
      J. Org. Chem., 57: 7241-7248 (1992).
      


1762. Tanaka, H., Takashima, H., Ubasawa, M., Sekiya, K., Nitta, I., Baba, M., Shigeta, S., Walker, R.T., De Clercq, E. & Miyasaka, T.
      Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio))thymine (HEPT) as potent and selective anti-HIV-1 agents.
      J. Med. Chem., 35: 4713-4719 (1992).
      


1763. Baba, M., Debyser, Z., Shigeta, S. & De Clercq, E.
      Highly potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by the HIV-1-specific reverse transcriptase inhibitors.
      Drugs of the Future, 17: 891-897 (1992).
      


1764. De Clercq, E. & Snoeck, R.
      a) Nouvelles acquisitions dans le domaine des antiviraux (anti-VIH).
      J. Pharm. Belg., 47: 317-322 (1992).
      b) Nieuwe ontwikkelingen op het gebied van antivirale (anti-HIV) middelen.
      Farmaceutisch Tijdschrift voor België, 69: 202-206 (1992).
      


1765. De Clercq, E.
      Human immunodeficiency virus inhibitors targeted at virus-cell fusion and/or viral uncoating.
      Int. J. Immunotherapy, 8: 115-123 (1992).
      


1766. Snoeck, R., Schols, D., Sadzot-Delvaux, C., Cloes, J.M., Andrei, G., De Clercq, E., Piette, J. & Rentier, B.
      Flow cytometric method for the detection of gpI antigens of varicella zoster virus and evaluation of anti-VZV agents.
      J. Virol. Methods, 38: 243-254 (1992).
      


1767. Witvrouw, M., Pauwels, R., Vandamme, A.-M., Schols, D., Reymen, D., Yamamoto, N., Desmyter, J. & De Clercq, E.
      Cell type-specific anti-human immunodeficiency virus type 1 activity of the transactiva­tion inhibitor Ro5-3335.
      Antimicrob. Agents Chemother., 36: 2628-2633 (1992).
      


1768. Neyts, J., Snoeck, R. & De Clercq, E.
      Therapy for herpesvirus infections.
      Current Opinion in Infectious Diseases, 5: 816-826 (1992).
      


1769. Schols, D. & De Clercq, E.
      Anti-HIV agents interfering with the viral gp120-cellular CD4 interaction.
      Proceedings of the Third International Symposium on Molecular Aspects of Chemothe­rapy, Gdansk, Poland, 19-21 June 1991.
      In "Molecular Aspects of Chemotherapy", D. Shugar, W. Rode & E. Borowski (eds.). Polish Scientific Publishers PWN Ltd, Warszawa, Poland, pp. 187-208 (1992).
      


1770. Herdewijn, P. & De Clercq, E.
      Future applications of oligonucleotides in antiviral and antitu­moral chemotherapy.
      In "Medicinal Chemistry for the 21st Century", C.G. Wermuth (ed.). Blackwell Scientific Publishers, pp. 45-60 (1992).
      


1771. Balzarini, J. & De Clercq, E.
      Assay method for monitoring the inhibitory effects of antimetabo­lites on the activity of inosinate dehydrogenase in intact human CEM lymphocyte cells.
      Biochem. J., 287: 785-790 (1992).
      


1772. Tronchet, J.M.J., Iznaden, M., Barbalat-Rey, F., Dhimane, H., Ricca, A., Balzarini, J. & De Clercq, E.
      Isoxazolidine analogs of nucleosides.
      Eur. J. Med. Chem., 27: 555-560 (1992).
      


1773. Ding, L., Balzarini, J., Schols, D., Meunier, B. & De Clercq, E.
      Anti-human immunodeficiency virus effects of cationic metalloporphyrin-ellipticine complexes.
      Biochem. Pharmacol., 44: 1675-1679 (1992).
      


1774. Witvrouw, M., Schols, D., Andrei, G., Snoeck, R., Ikeda, S., Pauwels, R., Van Schepdael, A., Arnout, J., Claes, P., Desmyter, J. & De Clercq, E.
      New polyacetal polysulphate active against human immunodeficiency virus and other enveloped viruses.
      Antiviral Chem. Chemother., 3: 351-360 (1992).
      


1775. Naesens, L., Balzarini, J. & De Clercq, E.
      Pharmacokinetics in mice of the anti-retrovirus agent 9-(2-phosphonyl­methoxyethyl)adenine.
      Drug Metab. Dispos., 20: 747-752 (1992).
      


1776. Herdewijn, P., Kerremans, L., Snoeck, R., Van Aerschot, A., Esmans, E. & De Clercq, E.
      Synthesis and anti-herpes activity of 5-trifluorovinyl-2'-deoxyuridine.
      Bioorganic Med. Chem. Lett. 2: 1057-1062 (1992).
      


1777. Patil, S.D., Schneller, S.W., Hosoya, M., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral properties of (±)-5'-noraristeromycin and related purine carbo­cyclic nucleosides. A new lead for anti-human cytomegalovirus agent design.
      J. Med. Chem., 35: 3372-3377 (1992).
      


1778. Bergstrom, D.E., Mott, A.W., De Clercq, E., Balzarini, J. and Swartling, D.J.
      3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-de­oxythymidine.
      J. Med. Chem., 35: 3369-3372 (1992).
      


1779. de la Cruz, A., Elguero, J., Goya, P., Martinez, A., Gotor, V., Moris, F. & De Clercq, E.
      Synthesis and antiviral evaluation of new 4-quinolone acyclonu­cleosides.
      J. Chem. Res. (S): 216-217; (M): 1682-1693 (1992).
      


1780. Pérez-Pérez, M.-J., Balzarini, J., Hosoya, M., De Clercq, E. & Camarasa, M.-J.
      Synthesis of adamantane spiro sulfones as potential antiviral agents.
      Bioorganic Med. Chem. Lett., 2: 647-648 (1992).
      


1781. Joos, P.E., Esmans, E.L., Dommisse, R.A., De Bruyn, A., Balzarini, J. & De Clercq, E.
      123. Synthesis and biological evaluation of 2-(2-deoxy-ß-D-ribofuranosyl)pyridine-4-carboxamide.
      Helv. Chim. Acta, 75: 1613-1620 (1992).
      


1782. Van Maarseveen, J.H., Hermkens, P.H.H., De Clercq, E., Balzarini, J., Scheeren, H.W. and Kruse, C.G.
      Antiviral and antitumor structure-activity relationship studies on tetracyclic eudisto­mines.
      J. Med. Chem., 35: 3223-3230 (1992).
      


1783. Balzarini, J., Pérez-Pérez, M.-J., San-Félix, A., Camarasa, M.-J., Barr, P.J. & De Clercq, E.
      Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-bu­tyldimethylsilyl)-ß-D-ri­bofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-di-oxide)thymine (TSAO-T).
      J. Biol. Chem., 267: 11831-11838 (1992).
      


1784. Debyser, Z., Vandamme, A.-M., Pauwels, R., Baba, M., Desmyter, J. & De Clercq, E.
      Kinetics of inhibition of endogenous human immunodeficiency virus type 1 reverse transcription by 2',3'-dideoxynucleoside 5'-triphosphate, tetrahydroimidazo-[4,5,1-jk][1,4]-benzodiazepin-2(1H)-thione, and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)-thymine derivatives.
      J. Biol. Chem., 267: 11769-11776 (1992).
      


1785. Mrani, D., Gosselin, G., Bailly, C., Houssin, R., Rao, K.E., Zimmermann, J., Balzarini, J., De Clercq, E., Hénichart, J.-P., Imbach, J.-L. & Lown, J.W.
      Synthesis, determination of sequence selective DNA minor groove binding and biological evaluation of hybrid bithiazole-linked netropsin derivatives.
      Eur. J. Med. Chem., 27: 331-344 (1992).
      


1786. Hiebl, J., Zbiral, E., Balzarini, J. & De Clercq, E.
      Side-chain derivatives of biologically active nucleosides. 1. Side-chain analogs of 3'-azido-3'-deoxythymidine (AZT).
      J. Med. Chem., 35: 3016-3023 (1992).
      


1787. Pérez-Pérez, M.-J., San-Félix, A., Balzarini, J., De Clercq, E. & Camarasa, M.-J.
      TSAO analogues. Stereospecific synthesis and anti-HIV-1 activity of 1-[2',5'-bis-O-(tert-butyldimethylsilyl)-ß-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-di­oxide)pyrimidine and pyrimidine-modified nucleosides.
      J. Med. Chem., 35: 2988-2995 (1992).
      


1788. Mullah, K.B., Rao, T.S., Balzarini, J., De Clercq, E. & Bentrude, W.G.
      Potential prodrug derivatives of 2',3'-didehydro-2',3'-dideoxynucleosides. Preparations and antiviral activities.
      J. Med. Chem., 35: 2728-2735 (1992).
      


1789. Camarasa, M.-J., Pérez-Pérez, M.-J., San-Félix, A., Balzarini, J. & De Clercq, E.
      3'-Spiro nucleosides, a new class of specific human immunodefi­ciency virus type 1 inhibitors: synthesis and an­tiviral activity of [2',5'-bis-O-(tert-butyldimethylsilyl)-ß-D-xylo- and -ribofu­ranose]-3'-spiro-5"-[4"-amino-1",2"-oxathiole 2",2"-dioxide] (TSAO) pyrimidine nucleosides.
      J. Med. Chem., 35: 2721-2727 (1992).
      


1790. De Clercq, E., Yamamoto, N., Pauwels, R., Baba, M., Schols, D., Nakashima, H., Balza­rini, J., Debyser, Z., Murrer, B.A., Schwartz, D., Thornton, D., Bridger, G., Fricker, S., Henson, G., Abrams, M. & Picker, D.
      Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event.
      Proc. Natl. Acad. Sci. USA, 89: 5286-5290 (1992).
      


1791. Debyser, Z., De Vreese, K., Pauwels, R., Yamamoto, N., Anné, J., De Clercq, E. & Desmyter, J.
      Differential inhibitory effects of TIBO derivatives on different strains of simian immu­nodeficiency virus.
      J. Gen. Virol., 73: 1799-1804 (1992).
      


1792. Lim, B.B., Marquez, V.E., Dobyns, K.A., Cooney, D.A. & De Clercq, E.
      Synthesis and biological study of the cyclopentenyl carbocyclic nucleoside analogue of 5-azacytidine.
      Nucleosides & Nucleotides, 11: 1123-1135 (1992).
      


1793. Fedorov, I.I., Kazmina, E.M., Novicov, N.A., Gurskaya, G.V., Bochkarev, A.V., Jasko, M.V., Victorova, L.S. Kukhanova, M.K., Krayevsky, A.A., Balzarini, J. & De Clercq, E.
      Synthesis, structure and some biological properties of 3'-C-branched 2'-deoxythymidines and their 5'-phosphate derivatives.
      Khimiko-Farmatsevtischeskii Zhurnal, 26: 14-24 (1992).
      


1794. Tolstikov, V.V., Holpne Kozlova, N.V., Oreshkina, T.D., Osipova, T.V., Preobrazhen­skaya, M.N., Sztaricskai, F., Balzarini, J. & De Clercq, E.
      Amides of antibiotic streptonigrin and amino dicarboxylic acids or aminosugars: synthe­sis and biological evaluation.
      J. Antibiotics, 45: 1020-1025 (1992).
      


1795. Tolstikov, V.V., Preobrazhenskaya, M.N., Balzarini, J. & De Clercq, E.
      Chemical modification of antibiotic streptonigrin: synthesis and properties of 2'-decar­boxy-2'-aminostreptonigrin (streptonigrone-2'-imine).
      J. Antibiotics, 45: 1002-1004 (1992).
      


1796. Robins, M.J., Samano, V., Zhang, W., Balzarini, J., De Clercq, E., Borchardt, R.T., Lee, Y. & Yuan, C.-S.
      Nucleic acid related compounds. 74. Synthesis and biological ac­tivity of 2'(and 3')-de­oxy-2'(and 3')-methylenenucleoside ana­logues that function as mechanism-based inhibi­tors of S-adenosyl-L-homocysteine hydrolase and/or ribonucleotide reductase.
      J. Med. Chem., 35: 2283-2293 (1992).
      


1797. Patil, S.D., Koga, M., Schneller, S.W., Snoeck, R. & De Clercq, E.
      (±)-Carbocyclic 5'-nor-2'-deoxyguanosine and related purine derivatives: synthesis and antiviral properties.
      J. Med. Chem., 35: 2191-2195 (1992).
      


1798. De Clercq, E.
      New perspectives for the chemotherapy and chemoprophylaxis of AIDS (acquired immune deficiency syndrome).
      Verh. K. Acad. Geneeskd. Belg., 54: 57-89 (1992).
      


1799. De Clercq, E.
      Novel molecular target for highly specific inhibitors of HIV-1 reverse transcriptase.
      In "New Leads and Targets in Drug Research", P. Krogsgaard-Larsen, S. Brogger Christensen & H. Kofod (eds.). Alfred Benzon Symposium 33. Munksgaard, Copenha­gen, Denmark, pp. 81-95 (1992).
      


1800. Schols, D., Pauwels, R., Desmyter, J. & De Clercq, E.
      Presence of class II histocompatibility DR proteins on the envelope of human immu­nodeficiency virus demonstrated by FACS analysis.
      Virology, 189: 374-376 (1992).
      


1801. Neyts, J., Snoeck, R., Schols, D., Balzarini, J., Esko, J.D., Van Schepdael, A. & De Clercq, E.
      Sulfated polymers inhibit the interaction of human cytomegalovirus with cell surface heparan sulfate.
      Virology, 189, 48-58 (1992).
      


1802. Debyser, Z., Pauwels, R., Baba, M., Desmyter, J. & De Clercq, E.
      Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine deriva­tives with the human immunodeficiency virus type 1 reverse transcriptase.
      Mol. Pharmacol., 41: 963-969 (1992).
      


1803. Neyts, J., Snoeck, R., Wutzler, P., Cushman, M., Klöcking, R., Helbig, B., Wang, P. & De Clercq, E.
      Poly(hydroxy)carboxylates as selective inhibitors of cy­tomegalovirus and herpes sim­plex virus replication.
      Antiviral Chem. & Chemother., 3: 215-222 (1992).
      


1804. Baraldi, P.G., Manfredini, S., Simoni, D., Aghazadeh Tabrizi, M., Balzarini, J. & De Clercq, E.
      Geiparvarin analogues. 3. Synthesis and cytostatic activity of 3(2H)-furanone and 4,5-dihydro-3(2H)-furanone congeners of geiparvarin, containing a geraniol-like fragment in the side chain.
      J. Med. Chem., 35: 1877-1882 (1992).
      


1805. De Clercq, E., Walker, R.T. & Whale, R.F.
      3'-O-Benzyl-(E)-5-(2-bromovinyl)-2'-deoxyuridine is active as an anti-herpes agent in vivo but not in vitro.
      Med. Chem. Res., 2: 111-118 (1992).
      


1806. Balzarini, J., Pérez-Pérez, M.-J., San-Félix, A., Schols, D., Perno, C.-F., Vandamme, A.-M., Camarasa, M.-J. & De Clercq, E.
      2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxathiole-2",2"-di­oxide)pyrimidine (TSAO) nucleoside analogues: highly selective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase.
      Proc. Natl. Acad. Sci. USA, 89: 4392-4396 (1992).
      


1807. Pérez-Pérez, M.-J., San-Félix, A., Camarasa, M.-J., Balzarini, J. & De Clercq, E.
      Synthesis of [1-[2',5'-bis-O-(t-butyldimethylsilyl)-ß-D-xylo- and ß-D-ribofurano­syl]thymine]-3'-spiro-5"-[4"-amino-1",2"-oxathiole-2",2"-dioxide] (TSAO). A novel type of specific anti-HIV agents.
      Tetrahedron Letters, 33: 3029-3032 (1992).
      


1808. Debyser, Z., Pauwels, R., Andries, K. & De Clercq, E.
      Specific HIV-1 reverse transcriptase inhibitors.
      J. Enzyme Inhibition, 6: 47-53 (1992).
      


1809. Shimizu, S.I., Balzarini, J., De Clercq, E. & Walker, R.T.
      The synthesis and biological properties of some aryl bis(nucleosid-5'-yl)phosphates using nucleosides with proven anti-HIV activity.
      Nucleosides & Nucleotides, 11: 583-594 (1992).
      


1810. Tanaka, H., Miyasaka, T., Sekiya, K., Takashima, H., Ubasawa, M., Nitta, I., Baba, M., Walker, R.T. & De Clercq, E.
      Synthesis of some analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) which have different types of acyclic structures.
      Nucleosides & Nucleotides, 11: 447-456 (1992).
      


1811. De Clercq, E.
      Antivirale chemotherapie.
      In "Medische Virologie" (vijfde, herziene druk), J.B. Wilterdink (red.). Bohn Stafleu Van Loghum, Houten, Antwerp, pp. 345-366 (1992).
      


1812. Balzarini, J., Neyts, J., Schols, D., Hosoya, M., Van Damme, E., Peumans, W. & De Clercq, E.
      The mannose-specific plant lectins from Cymbidium hybrid and Epi­pactis helleborine and the (N-acetylglucosamine)n-specific plant lectin from Urtica dioica are potent and selective inhibitors of human immunodeficiency virus and cytomegalovirus replication in vitro.
      Antiviral Res., 18: 191-207 (1992).
      


1813. De Vreese, K., Debyser, Z., Pauwels, R., Desmyter, J., De Clercq, E. & Anné, J.
      Resistance of human immunodeficiency virus type 1 reverse transcriptase to TIBO derivatives induced by site-directed mutagenesis.
      Virology, 188: 900-904 (1992).
      


1814. Balzarini, J., Perez-Perez, M.-J., San-Felix, A., Velazquez, S., Camarasa, M.-J. & De Clercq, E.
      [2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5"-[4"-amino-1",2"-oxathiole-2",2"-di­oxide) (TSAO) derivatives of purine and pyrimidine nucleosides as potent and selective inhibitors of hu­man immunodeficiency virus type 1.
      Antimicrob. Agents Chemother., 36: 1073-1080 (1992).
      


1815. Mohan, P., Schols, D., Baba, M. & De Clercq, E.
      Sulfonic acid polymers as a new class of human immunodeficiency virus inhibitors.
      Antiviral Res., 18: 139-150 (1992).
      


1816. Neyts, J., Balzarini, J., Naesens, L. & De Clercq, E.
      Efficacy of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine and 9-(1,3-dihy­droxy-2-propoxymethyl)guanine for the treatment of murine cytomegalovirus infection in severe combined immunodefi­ciency mice.
      J. Med. Virol., 37: 67-71 (1992).
      


1817. Shigeta, S., Mori, S., Baba, M., Ito, M., Honzumi, K., Nakamura, K., Oshitani, H., Numazaki, Y., Matsuda, A., Obara, T., Shuto, S. & De Clercq, E.
      Antiviral activities of ribavirin, 5-ethynyl-1-ß-D-ribofuranosylimidazole-4-carboxamide and 6'-(R)-6'-C-methyl-neplanocin A against several ortho- and paramyxoviruses.
      Antimicrob. Agents Chemother., 36: 435-439 (1992).
      


1818. Naesens, L., Balzarini, J. & De Clercq, E.
      Acyclic adenine nucleoside phosphonates in plasma determined by high-performance liquid chromatography with fluorescence detection.
      Clin. Chem., 38: 480-485 (1992).
      


1819. Vandendriessche, F., Snoeck, R., Janssen, G., Hoogmartens, J., Van Aerschot, A., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of acyclic nucleosides with a 3(S),5-dihydroxypentyl or 4(R)-methoxy-3(S),5-dihydroxypentyl side chain.
      J. Med. Chem., 35: 1458-1465 (1992).
      


1820. Shigeta, S., Mori, S., Baba, M., Hosoya, M., Mochizuki, N., Chiba, T. & De Clercq, E.
      Inhibitory effect of pyridobenzoazoles on orthomyxo- and paramyxovirus replication in vitro.
      Antiviral Chem. Chemother., 3: 171-177 (1992).
      


1821. Dolnak, D.R., Munguia, D., Wiley, C.A., De Clercq, E., Bergeron-Lynn, G.L., Boscher, C., Connor, J.D., Sherwood, C., Capparelli, E., Armani, R. & Freeman, W.R.
      Lack of retinal toxicity of the anticytomegalovirus drug (S)-1-(3-hydroxy-2-phosphonyl­methoxypropyl)cytosine.
      Invest. Ophthalmol. Vis. Sci., 33: 1557-1563 (1992).
      


1822. Andrei, G., Snoeck, R., Goubau, P., Desmyter, J. & De Clercq, E.
      Comparative activity of various compounds against clinical strains of herpes simplex virus.
      Eur. J. Clin. Microbiol. Infect. Dis., 11: 143-151 (1992).
      


1823. De Clercq, E.
      HIV inhibitors targeted at the reverse transcriptase.
      AIDS Res. Human Retrovir., 8: 119-134 (1992).
      


1824. Perno, C.-F., Yarchoan, R., Balzarini, J., Bergamini, A., Milanese, G., Pauwels, R., De Clercq, E., Rocchi, G. & Calio, R.
      Different pattern of activity of inhibitors of the human immunodeficiency virus in lym­phocytes and monocyte/macrophages.
      Antiviral Res., 17: 289-304 (1992).
      


1825. Baba, M., Shigeta, S., Tanaka, H., Miyasaka, T., Ubasawa, M., Umezu, K., Walker, R.T., Pauwels, R. & De Clercq, E.
      Highly potent and selective inhibition of HIV-1 replication by 6-phenylthiouracil deriva­tives.
      Antiviral Res., 17: 245-264 (1992).
      


1826. Schols, D., Pauwels, R., Witvrouw, M., Desmyter, J. & De Clercq, E.
      Differential activity of polyanionic compounds and castanosper­mine against HIV repli­cation and HIV-induced syncytium formation depending on virus strain and cell type.
      Antiviral Chem. & Chemother., 3: 23-29 (1992).
      


1827. Tanaka, H., Takashima, H., Ubasawa, M., Sekiya, K., Nitta, I., Baba, M., Shigeta, S., Walker, R.T., De Clercq, E. & Miyasaka, T.
      Structure-activity relationships of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine analogues: effect of substitutions at the C-6 phenyl ring and at the C-5 position on anti-HIV-1 activity.
      J. Med. Chem., 35: 337-345 (1992).
      


1828. Shuto, S., Obara, T., Toriya, M., Hosoya, M., Snoeck, R., Andrei, G., Balzarini, J. & De Clercq, E.
      New neplanocin analogues 1. Synthesis of 6'-modified neplanocin A derivatives as broad-spectrum antiviral agents.
      J. Med. Chem., 35: 324-331 (1992).
      


1829. Debyser, Z., Pauwels, R., Andries, K., Desmyter, J., Engelborghs, Y., Janssen, P.A.J. & De Clercq, E.
      Allosteric inhibition of human immunodeficiency virus type 1 reverse transcriptase by tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione compounds.
      Mol. Pharmacol., 41: 203-208 (1992).
      



107 publications in the year 1991



1830. Szinai, I., Veres, Zs., Ganzler, K., Hegedus-Vajda, J. & De Clercq, E.
      Metabolism of anti-herpes agent 5-(2-chloroethyl)-2'-deoxyuridine in mice and rats.
      Eur. J. Drug Metabolism Pharmacokinetics, 16: 129-136 (1991).
      


1831. Snoeck, R. & De Clercq, E.
      Mécanismes d'action et de résistance aux agents antiviraux.
      La Lettre de l'Infectiologue, 6: 507-510 (1991).
      


1832. De Clercq, E.
      Chemotherapy of the acquired immune deficiency syndrome (AIDS): acyclic nucleoside phosphonate analogues.
      Proceedings of the Satellite Meeting of the Fifth International Conference on Immuno­pharmacology, The International Symposium on Antivirals, Vaccines and Immunothe­rapy of HIV Infection, St. Petersburg, Florida, USA, 31 May-2 June 1991 (Eds. J.W. Hadden & M. Nonoyama).
      Int. J. Immunopharmacol., 13, Suppl. 1: 91-98 (1991).
      


1833. De Clercq, E.
      Chemotherapy of the acquired immune deficiency syndrome (AIDS): non-nucleoside in­hibitors of the human immunodeficiency virus type 1 reverse transcriptase.
      Proceedings of the Satellite Meeting of the Fifth International Conference on Immuno­pharmacology, The International Symposium on Antivirals, Vaccines and Immunothe­rapy of HIV Infection, St. Petersburg, Florida, USA, 31 May-2 June 1991 (Eds. J.W. Hadden & M. Nonoyama).
      Int. J. Immunopharmacol., 13, Suppl. 1: 83-89 (1991).
      


1834. Balzarini, J. & De Clercq, E.
      Conversion of acyclic nucleoside phosphonates to their diphosphate derivatives by 5-phosphoribosyl-1-pyrophosphate (PRPP) synthetase.
      In "Purine and Pyrimidine Metabolism in Man VII", Part A, R.A. Harkness, G. Elion and N. Zöllner (eds.). Plenum Press, New York, pp. 29-32 (1991).
      


1835. Nair, V., Buenger, G.S., Leonard, N.J., Balzarini, J. & De Clercq, E.
      Synthesis of 2',3'-dideoxy-3-isoadenosine: a new structural analogue of the anti-HIV ac­tive compound, 2',3'-dideoxyadenosine.
      J. Chem. Soc. Chem. Commun.: 1650-1651 (1991).
      


1836. Korolev, A.M., Lazko, E.I., Preobrazhenskaya, M.N., Balzarini, J. & De Clercq, E.
      Amides of anthracycline antibiotics and N-carboxymethylascorbigen.
      Khim. Pharm. Zhurnal., 25: 42-45 (1991).
      


1837. Andrei, G., Snoeck, R., Schols, D., Goubau, P., Desmyter, J. & De Clercq, E.
      Comparative activity of selected antiviral compounds against clinical isolates of human cytomegalovirus.
      Eur. J. Clin. Microbiol. Infect. Dis., 10: 1026-1033 (1991).
      


1838. Mrani, D., Gosselin, G., Auclair, C., Balzarini, J., De Clercq, E., Paoletti, C. & Imbach, J.-L.
      Synthesis, DNA binding, and biological activity of oxazolopyrido­carbazole-netropsin hybrid molecules.
      Eur. J. Med. Chem., 26: 481-488 (1991).
      


1839. Peters, M., Witvrouw, M., De Clercq, E. & Ruf, B.
      Pharmacokinetics of intravenous pentosan polysulphate (HOE/BAY 946) in HIV-positive patients.
      AIDS, 5: 1534-1535 (1991).
      


1840. Kohda, K., Ukai, H., Balzarini, J., De Clercq, E. & Torrence, P.F.
      Differential inhibition of retroviral reverse transcriptase by poly(2-fluoroadenylic acid), a template analogue.
      AIDS, 5: 341 (1991).
      


1841. Verberckmoes, F., Esmans, E.L., Dommisse, R.A., Lepoivre, J.A., Alderweireldt, F.C., Balzarini, J. & De Clercq,E.
      Synthesis and biological evaluation of some D-xylofuranosylpyridine C-nucleosides.
      Nucleosides & Nucleotides, 10: 1771-1787 (1991).
      


1842. Mikhailopulo, I.A., Sivets, G.G., Pricota, T.I., Poopeiko, N.E., Balzarini, J. & De Clercq, E.
      Synthesis and biological properties of 2-amino-3-fluoro-2,3-dideoxy-D-pentofuranosides of natural heterocyclic bases.
      Nucleosides & Nucleotides, 10: 1743-1757 (1991).
      


1843. Sági, J., Szabolcs, A., Ebinger, K., Ötvös, L., Balzarini, J. & De Clercq, E.
      Effect of 2-amino substitution on the antiviral effects of 5-ethyl-2'-deoxyuridine and (E)-5-(2-bromovinyl)-2'-deoxyuridine and their incorporation into DNA.
      Nucleosides & Nucleotides, 10: 1729-1742 (1991).
      


1844. Holmes, H.C., Mahmood, N., Karpas, A., Petrik, J., Kinchington, D., O'Connor, T., Jef­fries, D.J., Desmyter, J., De Clercq, E., Pauwels, R. & Hay, A.
      Screening of compounds for activity against HIV: a collaborative study.
      Antiviral Chem. Chemother., 2: 287-293 (1991).
      


1845. Shuto, S., Obara, T. & De Clercq, E.
      New neplanocin analogues. Synthesis and antiviral activity of 6'-modified neplanocin A derivatives.
      Nucleic Acids Symposium Series, 25: 7-8 (1991).
      


1846. Kukla, M.J., Breslin, H.J., Diamond, C.J., Grous, P.P., Ho, C.Y., Miranda, M., Rodgers, J.D., Sherrill, R.G., De Clercq, E., Pauwels, R., Andries, K., Moens, L.J., Janssen, M.A.C. & Janssen, P.A.J.
      Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methyl-imidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) derivatives.
      J. Med. Chem., 34, 3187-3197 (1991).
      


1847. Balzarini, J., Lee, C.-K., Herdewijn, P. & De Clercq, E.
      Mechanism of the potentiating effect of ribavirin on the activity of 2',3'-dideoxyinosine (ddIno) against human immunodeficiency virus.
      J. Biol. Chem., 266: 21509-21514 (1991).
      


1848. Hosoya, M., Balzarini, J., Shigeta, S. & De Clercq, E.
      Differential inhibitory effects of sulfated polysaccharides and polymers on the replication of various myxoviruses and retroviruses, depending on the composition of the target amino acid sequences of the viral envelope glycoproteins.
      Antimicrob. Agents Chemother., 35: 2515-2520 (1991).
      


1849. De Clercq, E.
      Overzicht van de antivirale geneesmiddelen gebruikt in de behandeling van herpesvirus­infecties.
      In "Kliniek en Behandeling van Herpesvirus Infecties", P.J. van den Broek, R. van Furth & H.T. Weiland (eds.). Boerhaave Com­missie voor Postacademisch Onderwijs in de Geneeskunde, Faculteit der Geneeskunde, Rijksuniversiteit Leiden, The Netherlands, pp. 29-43 (1991).
      


1850. De Clercq, E.
      Therapy for herpesvirus infections.
      In "Current Opinion in Infectious Diseases, Antimicrobial Agents: Viral/Parasitic", R.G. Douglas Jr. & N. Clumeck (eds.), vol. 4, pp. 795-803. Current Science (1991).
      


1851. Simoni, D., Manfredini, S., Aghazadeh Tabrizi, M., Bazzanini, R., Baraldi, P.G., Balza­rini, J. & De Clercq, E.
      Geiparvarin analogues. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates.
      J. Med. Chem., 34: 3172-3176 (1991).
      


1852. Lin, J.-C., De Clercq, E. & Pagano, J.S.
      Inhibitory effects of acyclic nucleoside phosphonate analogs, including (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, on Epstein-Barr virus replication
      Antimicrob. Agents Chemother., 35: 2440-2443 (1991).
      


1853. Stals, F.S., De Clercq, E. & Bruggeman, C.A.
      Comparative activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine and 9-(1,3-dihydroxy-2-propoxymethyl)guanine against rat cytomegalovirus infection in vitro and in vivo.
      Antimicrob. Agents Chemother., 35: 2262-2266 (1991).
      


1854. De Clercq, E.
      Huidige therapeutische mogelijkheden bij AIDS
      Tijdschr. voor Geneeskunde, 47: 1559-1566 (1991).
      


1855. Neyts, J., Snoeck, R., Schols, D., Himpens, B. & De Clercq, E.
      Sensitive, reproducible and convenient fluorometric assay for the in vitro evaluation of anti-cytomegalovirus agents.
      J. Virol. Methods, 35: 27-38 (1991).
      


1856. Snoeck, R. & De Clercq, E.
      (S)-1-(3-Hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC), a potent and selec­tive inhibitor of cytomegalovirus infection in vitro and in vivo.
      Proc. 23rd Int. Course on Transplantation and Clinical Immuno­logy, Lyon, France, June 3-5, 1991.
      In "Transplantation and Clinical Immunology XXIII", J.L. Touraine et al. (eds.). Elsevier Science Publishers B.V., Amsterdam, The Netherlands, pp. 169-176 (1991).
      


1857. Snoeck, R., Holý, A., Rosenberg, I. & De Clercq, E.
      Inhibition of cytomegalovirus replication by acyclic nucleoside phosphonate analogues: structure-activity relationship.
      Proceedings of the "3rd International Cytomegalovirus Workshop", Bologna, Italy, 11-14 June 1991.
      In "Progress in Cytomegalovirus Research", M.P. Landini (ed.). Elsevier Science Publishers B.V., Amsterdam, The Netherlands, pp. 337-340 (1991).
      


1858. Andrei, G., Snoeck, R. & De Clercq, E.
      Infection of different human tumor cell lines by human cytomegalovirus.
      Proceedings of the "3rd International Cytomegalovirus Workshop", Bologna, Italy, 11-14 June 1991.
      In "Progress in Cytomegalovirus Research", M.P. Landini (ed.). Elsevier Science Publishers B.V., Amsterdam, The Netherlands, pp. 271-274 (1991).
      


1859. Hosoya, M., Neyts, J., Yamamoto, N., Schols, D., Snoeck, R., Pauwels, R. & De Clercq, E.
      Inhibitory effects of polycations on the replication of enveloped viruses (HIV, HSV, CMV, RSV, influenza A virus and togaviruses) in vitro.
      Antiviral Chem. & Chemother., 2: 243-248 (1991).
      


1860. De Vos, E., Esmans, E.L., Lepoivre, J.A., Alderweireldt, F.C., Dommisse, R.A., François, P., Touillaux, R., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of 2-(2-deoxy-D-erythro-pent-1-enofurano­syl)pyridine C-nucleosides.
      Nucleosides & Nucleotides, 10: 1573-1598 (1991).
      


1861. Herdewijn, P., Van Aerschot, A., Busson, R., Claes, P. & De Clercq, E.
      Synthesis of 2'-deoxy-2'-fluoro-D-arabinopyranosyl nucleosides and their 3',4'-seco ana­logues.
      Nucleosides & Nucleotides, 10: 1525-1549 (1991).
      


1862. Hebel, D., Kirk, K.L., Kinjo, J., Kovács, T., Lesiak, K., Balzarini, J., De Clercq, E. & Torrence, P.F.
      Synthesis of a difluoromethylenephosphonate analogue of AZT 5'-triphosphate and its inhibition of HIV-1 reverse transcriptase.
      Bioorganic Med. Chem. Lett., 1: 357-360 (1991).
      


1863. Witvrouw, M., Schols, D., Andrei, G., Snoeck, R., Hosoya, M., Pauwels, R., Balzarini, J. & De Clercq, E.
      Antiviral activity of low-MW dextran sulphate (derived from dextran MW 1000) com­pared to dextran sulphate samples of higher MW.
      Antiviral Chem. & Chemother., 2: 171-179 (1991).
      


1864. De Clercq, E.
      Chemotherapy of viral infections.
      In "Medical Microbiology", 3rd ed., S. Baron (ed.). Churchill Livingstone Inc., New York. pp. 695-703 (1991).
      


1865. Lee, J.S., Mullaney, S., Bronson, R., Sharpe, A.H., Jaenisch, R., Balzarini, J., De Clercq, E. & Ruprecht, R.M.
      Transplacental antiretroviral therapy with 9-(2-phosphonylmethoxyethyl)adenine is embryotoxic in transgenic mice.
      J. Acquir. Immun. Defic. Syndr., 4: 833-838 (1991).
      


1866. Vanderhaeghe, H., Herdewijn, P. & De Clercq, E.
      15. Antibiotics and antiviral agents.
      In "A Textbook of Drug Design and Development", P. Krogsgaard-Larsen and H. Bund­gaard (eds.).
      Harwood Academic Publishers, London, pp. 531-605 (1991).
      


1867. Wigerinck, P., Pannecouque, C., Snoeck, R., Claes, P., De Clercq, E. & Herdewijn, P.
      5-(5-Bromothien-2-yl)-2'-deoxyuridine and 5-(5-chlorothien-2-yl)-2'-deoxyuridine are equipotent to (E)-5-(2-bromovinyl)-2'-deoxyuridine in the inhibition of herpes simplex virus type I replica­tion.
      J. Med. Chem., 34: 2383-2389 (1991).
      


1868. Boryski, J., Golankiewicz, B. & De Clercq, E.
      Synthesis and antiviral activity of 3-substituted derivatives of 3,9-dihydro-9-oxo-5H-imi­dazo[1,2-a]purines, tricyclic analogues of acyclovir and ganciclovir.
      J. Med. Chem., 34: 2380-2383 (1991).
      


1869. De Clercq, E.
      Broad-spectrum anti-DNA virus and anti-retrovirus activity of phosphonylmethoxyal­kylpurines and -pyrimidines.
      Biochem. Pharmacol., 42: 963-972 (1991).
      


1870. Balzarini, J., Lee, C.-K., Schols, D. & De Clercq, E.
      1-ß-D-Ribofuranosyl-1,2,4-triazole-3-carboxamide (ribavirin) and 5-ethynyl-1-ß-D-ri­bofuranosylimidazole-4-carboxamide (EICAR) markedly potentiate the inhibitory effect of 2',3'-dideoxyinosine on human immunodeficiency virus in peripheral blood lympho­cytes.
      Biochem. Biophys. Res. Commun., 178: 563-569 (1991).
      


1871. Atrazheva, E.D., Lukin, M.A., Jasko, M.V., Shushkova, T.V., Tarussova, N.B., Krayevsky, A.A., Balzarini, J. & De Clercq, E.
      2',3'-O-Cyclic derivatives of ribonucleosides and their 5'-phosphonates: synthesis and anti-HIV activity.
      Med. Chem. Res., 1: 155-165 (1991).
      


1872. Balzarini, J., Perno, C.-F., Schols, D. & De Clercq, E.
      Activity of acyclic nucleoside phosphonate analogues against human immunodeficiency virus in monocyte/macrophages and peripheral blood lymphocytes.
      Biochem. Biophys. Res. Commun., 178: 329-335 (1991).
      


1873. Palú, G., Stefanelli, S., Rassu, M., Parolin, C., Balzarini, J. & De Clercq, E.
      Cellular uptake of phosphonylmethoxyalkylpurine derivatives.
      Antiviral Res., 16: 115-119 (1991).
      


1874. De Castro, L.M., Kern, E.R., De Clercq, E., Ghaffar, A., Mayer, E.P., Vogt, P.E. & Gangemi, J.D.
      Phosphonylmethoxyalkyl purine and pyrimidine derivatives for treatment of opportunis­tic cytomegalovirus and herpes simplex virus infections in murine AIDS.
      Antiviral Res., 16: 101-114 (1991).
      


1875. Maudgal, P.C. & De Clercq, E.
      Effects of phosphonylmethoxyalkyl-purine and -pyrimidine deriva­tives on TK+ and TK- HSV-1 keratitis in rabbits.
      Antiviral Res., 16: 93-100 (1991).
      


1876. Del Gobbo, V., Foli, A., Balzarini, J., De Clercq, E., Balestra, E., Villani, N., Marini, S., Perno, C.F. & Calio, R.
      Immunomodulatory activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA), a potent anti-HIV nucleotide analogue, on in vivo murine models.
      Antiviral Res., 16: 65-75 (1991).
      


1877. Naesens, L., Balzarini, J. & De Clercq, E.
      Single-dose administration of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the prophylaxis of retrovirus infection in vivo.
      Antiviral Res., 16: 53-64 (1991).
      


1878. Neyts, J., Snoeck, R., Balzarini, J. & De Clercq, E.
      Particular characteristics of the anti-human cytomegalovirus activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC) in vitro.
      Antiviral Res., 16: 41-52 (1991).
      


1879. Gordon, Y.J., Romanowski, E., Araullo-Cruz, T., Seaberg, L., Erzurum, S., Tolman, R. & De Clercq, E.
      Inhibitory effect of (S)-HPMPC, (S)-HPMPA, and 2'-nor-cyclic GMP on clinical ocular adenoviral isolates is serotype-dependent in vitro.
      Antiviral Res., 16: 11-16 (1991).
      


1880. Snoeck, R., Schols, D., Andrei, G., Neyts, J. & De Clercq, E.
      Antiviral activity of anti-cytomegalovirus agents (HPMPC, HPMPA) assessed by a flow cytometric method and DNA hybridization tech­nique.
      Antiviral Res., 16: 1-9 (1991).
      


1881. Holý, A., Balzarini, J., Snoeck, R. & De Clercq, E.
      Synthesis and antiviral evaluation of 9-(RS)-[2-phosphonylmethoxy-3-(2-pro­poxy)propyl]adenine.
      Int. J. Purine & Pyrimidine Res., 2: 61-65 (1991).
      


1882. Baba, M., Ito, M., Shigeta, S., Tanaka, H., Miyasaka, T., Ubasawa, M., Umezu, K., Walker, R.T. & De Clercq, E.
      Synergistic inhibition of human immunodeficiency virus type 1 replication by 5-ethyl-1-ethoxymethyl-6-(phenylthio)uracil (E-EPU) and azidothymidine in vitro.
      Antimicrob. Agents Chemother., 35: 1430-1433 (1991).
      


1883. Joos, P.E., Esmans, E.L., Dommisse, R.A., Van Dongen, W., Lepoivre, J.A., Alder­weireldt, F.C., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of 4-carbamoyl-2-ß-D-ribofuranosylpyridine.
      Nucleosides & Nucleotides, 10: 883-894 (1991).
      


1884. Mikhailopulo, I.A., Poopeiko, N.E., Pricota, T.I., Sivets, G.G., Kvasyuk, E.I., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral and cytostatic properties of 3'-deoxy-3'-fluoro- and 2'-azido-3'-fluoro-2',3'-dideoxy-D-ribofuranosides of natural heterocyclic bases.
      J. Med. Chem., 34: 2195-2202 (1991).
      


1885. Polsterer, J.-P., Zbiral, E., Balzarini, J. & De Clercq, E.
      Synthesis of L-threo and D-erythro-apiofuranosylcytidines.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 621-622 (1991).
      


1886. Van Aerschot, A., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of 1,4-dioxane, 1,4-oxathiane and 1,4-morpholine nu­cleoside analogues.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 591-592 (1991).
      


1887. Van Aerschot, A., Kerremans, L., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis and anti-HIV activity of dideoxycytidine analogues containing a pyranose car­bohydrate moiety.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 589-590 (1991).
      


1888. Wigerinck, P., Van Aerschot, A., De Clercq, E. & Herdewijn, P.
      5-(Thien-2-yl)-2'-deoxyuridine: a new and potent inhibitor of herpes simplex virus type 1 replication.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 585-586 (1991).
      


1889. Wigerinck, P., Van Aerschot, A., Kerremans, L., Balzarini, J., De Clercq, E., Claes, P. & Herdewijn, P.
      Synthesis of thymidine analogues with a cyanoimido substituent.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 583-584 (1991).
      


1890. Hiebl, J., Zbiral, E., Balzarini, J. & De Clercq, E.
      2,3'-Anhydro-[1-(6'-O-benzoyl-2',5'-dideoxy-ß-D-glucofuranosyl)thymine]. A versatile starting material for homonucleosides.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 521-522 (1991).
      


1891. Komiotis, D., Delatre, S., Holt, L., Ollapally, A.P., Balzarini, J., De Clercq, E. & Iigo, M.
      Biological important nucleosides: a general method for the syn­thesis of unsaturated ketonucleosides of uracil and its analogs.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 431-455 (1991).
      


1892. Tanaka, H., Baba, M., Hayakawa, H., Haraguchi, K., Miyasaka, T., Ubasawa, M., Taka­shima, H., Sekiya, K., Nitta, I., Walker, R.T. & De Clercq, E.
      Lithiation of uracil nucleosides and its application to the synthesis of a new class of anti-HIV-1 acyclonucleosides.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 397-400 (1991).
      


1893. De Clercq, E.
      Antiviral activity spectrum of nucleoside and nucleotide analogues.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 167-180 (1991).
      


1894. Herdewijn, P., Van Aerschot, A., Balzarini, J. & De Clercq, E.
      Synthesis of pyranose nucleosides.
      Proceedings of the "Ninth International Round Table on Nucleosides, Nucleotides and their Biological Applications", Uppsala, Sweden, 29 July-3 August 1990.
      Nucleosides & Nucleotides, 10: 119-127 (1991).
      


1895. Jansen, R.W., Molema, G., Pauwels, R., Schols, D., De Clercq, E. & Meijer, D.K.F.
      Potent in vitro anti-human immunodeficiency virus-1 activity of modified human serum albumins.
      Mol. Pharmacol., 39: 818-823 (1991).
      


1896. Baba, M., De Clercq, E., Tanaka, H., Ubasawa, M., Takashima, H., Sekiya, K., Nitta, I., Umezu, K., Walker, R.T., Mori, S., Ito, M., Shigeta, S. & Miyasaka, T.
      Highly potent and selective inhibition of human immunodeficiency virus type 1 by a novel series of 6-substituted acyclouridine derivatives.
      Mol. Pharmacol., 39: 805-810 (1991).
      


1897. Cools, M., Balzarini, J. & De Clercq, E.
      Mechanism of antiviral and cytotoxic action of (±)-6'ß-fluoroaristeromycin, a potent inhibitor of S-adenosylhomocysteine hydrolase.
      Mol. Pharmacol., 39: 718-724 (1991).
      


1898. Schols, D., Wutzler, P., Klöcking, R., Helbig, B. & De Clercq, E.
      Selective inhibitory activity of polyhydroxycarboxylates derived from phenolic com­pounds against human immunodeficiency virus replication.
      J. Acquir. Immun. Defic. Syndr., 4: 677-685 (1991).
      


1899. Maudgal, P.C. & De Clercq, E.
      (S)-1-(3-Hydroxy-2-phosphonylmethoxypropyl)cytosine in the the­rapy of thymidine kinase-positive and -deficient herpes simplex virus experimental keratitis.
      Invest. Ophthalmol. Visual Sci., 32: 1816-1820 (1991).
      


1900. Balzarini, J., Holý, A., Jindrich, J., Dvorakova, H., Hao, Z., Snoeck, R., Herdewijn, P., Johns, D.G. & De Clercq, E.
      9-[(2RS)-3-fluoro-2-phosphonylmethoxypropyl] derivatives of purines: a class of highly selective antiretroviral agents in vitro and in vivo.
      Proc. Natl. Acad. Sci. USA, 88: 4961-4965 (1991).
      


1901. Olsufyeva, E.N., Backinowsky, L.V., Preobrazhenskaya, M.N., Balzarini, J. & De Clercq, E.
      New analogues of anthracycline antibiotics containing 2,3,6-trideoxy-3-amino-3-C-methyl-L-arabino-hexose (L-eremosamine).
      Bioorganicheskaya Khimia, 17: 548-555 (1991).
      Soviet Journal of Bioorganic Chemistry, 17: 316-322 (1991).
      


1902. de Vries, E., Stam, J.G., Franssen, F.F.J., Nieuwenhuijs, H., Chavalitshewinkoon, P., De Clercq, E., Overdulve, J.P. & van der Vliet, P.C.
      Inhibition of the growth of Plasmodium falciparum and Plasmodium berghei by the DNA polymerase inhibitor HPMPA.
      Molec. Biochem. Parasitol., 47: 43-50 (1991).
      


1903. Balzarini, J. & De Clercq, E.
      5-Phosphoribosyl 1-pyrophosphate synthetase converts the acyclic nucleoside phos­phonates 9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonyl­methoxyethyl)adenine directly to their antivirally active diphosphate derivatives.
      J. Biol. Chem., 266: 8686-8689 (1991).
      


1904. Wigerinck, P., Snoeck, R., Claes, P., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of 5-heteroaryl-substituted-2'-deoxyuridines.
      J. Med. Chem., 34: 1767-1772 (1991).
      


1905. Herdewijn, P.A.M., Van Aerschot, A., Balzarini, J., De Clercq, E., Everaert, D.H., De Winter, H.L., Peeters, O.M., Blaton, N.M. & De Ranter, C.J.
      3'-Fluoro- and 3'-azido-substituted 2',3'-dideoxynucleosides: structure-activity relation­ship.
      Med. Chem. Res., 1: 9-19 (1991).
      


1906. Ito, M., Baba, M., Shigeta, S., De Clercq, E., Walker, R.T., Tanaka, H. & Miyasaka, T.
      Synergistic inhibition of human immunodeficiency virus type 1 (HIV-1) replication in vitro by 1-[(2-hydroxyethoxy)methyl]-6-phenylthiothymine (HEPT) and recombinant alpha interferon.
      Antiviral Res., 15: 323-330 (1991).
      


1907. Snoeck, R. & De Clercq, E.
      Drogues anti-VIH en cours de développement.
      - In "SIDA", S. Blanche, P.-M. Girard, C. Katlama, G. Pialoux &
      A.-G. Saimot (eds.). Doin Editeurs, Paris, France, pp. 349-357 (1991).
      - Editions Techniques, Encycl. Méd. Chir., Paris France, 25132 C10, 4 p. (1991).
      


1908. Debart, F., Gosselin, G., Rayner, B., Le Ber, P., Auclair, C., Balzarini, J., De Clercq, E., Paoletti, C. & Imbach, J.-L.
      Synthesis, DNA binding properties and biological evaluation of novel oligo-meta-ben­zamides related to netropsin.
      Eur. J. Med. Chem., 26: 261-271 (1991).
      


1909. Maudgal, P.C. & De Clercq, E.
      Bromovinyldeoxyuridine treatment of herpetic keratitis clinically resistant to other antivi­ral agents.
      Current Eye Res., 10 (Suppl.): 193-199 (1991).
      


1910. Maudgal, P.C. & De Clercq, E.
      Efficacy of 9-(2-phosphonylmethoxyethyl)adenine in the therapy of TK+ and TK- herpes simplex virus experimental keratitis.
      Current Eye Res., 10 (Suppl.): 139-142 (1991).
      


1911. Schols, D., De Clercq, E., Witvrouw, M., Nakashima, H., Snoeck, R., Pauwels, R., Van Schepdael, A. & Claes, P.
      Sulphated cyclodextrins are potent anti-HIV agents acting syner­gistically with 2',3'-dideoxynucleoside analogues.
      Antiviral Chem. Chemother., 2: 45-53 (1991).
      


1912. De Clercq, E., Murase, J. & Marquez, V.E.
      Broad-spectrum antiviral and cytocidal activity of cyclopentenyl­cytosine, a carbocyclic nucleoside targeted at CTP synthetase.
      Biochem. Pharmacol., 41: 1821-1829 (1991).
      


1913. Tanaka, H., Baba, M., Saito, S., Miyasaka, T., Takashima, H., Sekiya, K., Ubasawa, M., Nitta, I., Walker, R.T., Nakashima, H. & De Clercq, E.
      Specific anti-HIV-1 "acyclonucleosides" which cannot be phosphorylated: synthesis of some deoxy analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine.
      J. Med. Chem., 34: 1508-1511 (1991).
      


1914. Hiebl, J., Zbiral, E., Balzarini, J. & De Clercq, E.
      Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-iso­cyano-2',3',5'-trideoxyuridine.
      J. Med. Chem., 34: 1426-1430 (1991).
      


1915. Tanaka, H., Baba, M., Ubasawa, M., Takashima, H., Sekiya, K., Nitta, I., Shigeta, S., Walker, R.T., De Clercq, E. & Miyasaka, T.
      Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted ana­logues of 1-[(2-hy­droxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).
      J. Med. Chem., 34: 1394-1399 (1991).
      


1916. Shiraki, K., Vonka, V., De Clercq, E. & Rapp, F.
      Selection of L cell sublines resistant to (E)-5-(2-bromovinyl)-2'-deoxyuridine.
      Intervirology, 32: 228-233 (1991).
      


1917. Baba, M., De Clercq, E., Tanaka, H., Ubasawa, M., Takashima, H., Sekiya, K., Nitta, I., Umezu, K., Nakashima, H., Mori, S., Shigeta, S., Walker, R.T. & Miyasaka, T.
      Potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by 5-ethyl-6-phenylthiouracil derivatives through their interaction with the HIV-1 reverse transcriptase.
      Proc. Natl. Acad. Sci. USA, 88: 2356-2360 (1991).
      


1918. Golankiewicz, B., Ostrowski, T., Boryski, J. & De Clercq, E.
      Synthesis of acyclowyosine and acyclo-3-methylguanosine, as probes for some chemical and biological properties resulting from the N-3 substitution of guanosine and its ana­logues.
      J. Chem. Soc. Perkin Trans. I: 589-593 (1991).
      


1919. Preobrazhenskaya, M.N., Bakina, E.V., Povarov, L.S., Lazhko, E.I., Aleksandrova, L.G., Balzarini, J. & De Clercq, E.
      Synthesis and cytostatic properties of daunorubicin derivatives, containing N-phenylthiourea or N-ethylthiourea moieties in the 3'-position.
      J. Antibiotics, 44: 192-199 (1991).
      


1920. De Clercq, E. & Holý, A.
      Efficacy of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine in various models of herpes simplex virus infection in mice.
      Antimicrob. Agents Chemother., 35: 701-706 (1991).
      


1921. De Clercq, E., Cools, M., Balzarini, J., Snoeck, R., Andrei, G., Hosoya, M., Shigeta, S., Ueda, T., Minakawa, N. & Matsuda, A.
      Antiviral activities of 5-ethynyl-1-ß-D-ribofuranosylimidazole-4-carboxamide and related compounds.
      Antimicrob. Agents Chemother., 35: 679-684 (1991).
      


1922. Kukla, M.J., Breslin, H.J., Pauwels, R., Fedde, C.L., Miranda, M., Scott, M.K., Sherrill, R.G., Raeymaekers, A., Van Gelder, J., Andries, K., Janssen, M.A.C., De Clercq, E. & Janssen, P.A.J.
      Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one (TIBO) deri-vatives.
      J. Med. Chem., 34: 746-751 (1991).
      


1923. De Clercq, E.
      Strategies in the development of selective antiviral agents.
      Actual. Chim. Thér., 18: 133-144 (1991).
      


1924. Rao, K.E., Krowicki, K., Balzarini, J., De Clercq, E., Newman, R.A. & Lown, J.W.
      Novel linked antiviral and antitumor agents related to netropsin - 2: Synthesis and bio­logical evaluation.
      Actual. Chim. Thér., 18: 21-42 (1991).
      


1925. Balzarini, J., Schols, D., Neyts, J., Van Damme, E., Peumans, W. & De Clercq, E.
      Ó-(1-3)- and Ó-(1-6)-D-mannose-specific plant lectins are markedly inhibitory to human immunodeficiency virus and cytomegalovirus infections in vitro.
      Antimicrob. Agents Chemother., 35: 410-416 (1991).
      


1926. Balzarini, J., Hao, Z., Herdewijn, P., Johns, D.G. & De Clercq, E.
      Intracellular metabolism and mechanism of anti-retrovirus action of 9-(2-phosphonyl­methoxyethyl)adenine, a potent anti-human immunodeficiency virus compound.
      Proc. Natl. Acad. Sci. USA, 88: 1499-1503 (1991).
      


1927. Debyser, Z., Pauwels, R., Andries, K., Desmyter, J., Kukla, M., Janssen, P.A.J. & De Clercq, E.
      An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione derivatives.
      Proc. Natl. Acad. Sci. USA, 88: 1451-1455 (1991).
      


1928. Shigeta, S., Konno, K., Baba, M., Yokota, T. & De Clercq, E.
      Comparative inhibitory effects of nucleoside analogues on different clinical isolates of human cytomegalovirus in vitro.
      J. Infect. Dis., 163: 270-275 (1991).
      


1929. Yokota, T., Mochizuki, S., Konno, K., Mori, S., Shigeta, S. & De Clercq, E.
      Inhibitory effects of selected antiviral compounds on human hepatitis B virus DNA syn­thesis.
      Antimicrob. Agents Chemother., 35: 394-397 (1991).
      


1930. De Clercq, E.
      Basic approaches to anti-retroviral treatment.
      J. Acquir. Immun. Defic. Syndr., 4: 207-218 (1991).
      


1931. Herranz, R., Castro-Pichel, J., García-López, M.T., Pérez, C., Balzarini, J. & De Clercq, E.
      Synthesis of 5'-N-(-amino-ß-mercaptoacyl)amino-5'-deoxynucleosides as potential antiviral compounds.
      Arch. Pharm., 324: 497-500 (1991).
      


1932. Tanaka, H., Baba, M., Hayakawa, H., Sakamaki, T., Miyasaka, T., Ubasawa, M., Taka­shima, H., Sekiya, K., Nitta, I., Shigeta, S., Walker, R.T., Balzarini, J. & De Clercq, E.
      A new class of HIV-1-specific 6-substituted acyclouridine deriva­tives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).
      J. Med. Chem., 34: 349-357 (1991).
      


1933. Cushman, M., Kanamathareddy, S., De Clercq, E., Schols, D., Gold­man, M.E. and Bowen, J.A.
      Synthesis and anti-HIV activities of low molecular weight aurin­tricarboxylic acid frag­ments and related compounds.
      J. Med. Chem., 34: 337-342 (1991).
      


1934. Cushman, M., Wang, P., Chang, S.H., Wild, C., De Clercq, E., Schols, D., Goldman, M.E. and Bowen, J.A.
      Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight.
      J. Med. Chem., 34: 329-337 (1991).
      


1935. Herranz, R., Castro-Pichel, J., García-López, M.T., Pérez, C., Balzarini, J. & De Clercq, E.
      Synthesis of penicillamine- and cysteine-containing nucleoamino acids as potential antivirals and aminopeptidase B inhibitors.
      J. Chem. Soc. Perkin Trans. I: 43-48 (1991).
      


1936. Balzarini, J., Naesens, L., Slachmuylders, J., Niphuis, H., Rosenberg, I., Holý, A., Schellekens, H. & De Clercq, E.
      9-(2-Phosphonylmethoxyethyl)adenine (PMEA) effectively inhibits retrovirus replication in vitro and simian immunodeficiency virus infection in rhesus monkeys.
      AIDS, 5: 21-28 (1991).
      



73 publications in the year 1990



1937. Shigeta, S. & De Clercq, E.
      Advances in the treatment of herpesvirus (herpes simplex virus and varicella-zoster virus) infections.
      Drugs of Today, 26: 29-39 (1990).
      


1938. Balzarini, J., Van Aerschot, A., Herdewijn, P. & De Clercq, E.
      Potent and selective anti-HIV activity of 5-chloro-substituted derivatives of 3'-azido-2',3'-dideoxycytidine, 3'-fluoro-2',3'-dideoxycytidine, and 2',3'-didehydro-2',3'-dideoxy­cytidine.
      Ann. N.Y. Acad. Sci., 616: 480-482 (1990).
      


1939. Iigo, M., Nishikata, K.-i., Nakajima, Y., Hoshi, A. & De Clercq, E.
      Effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine on life-span and 5-fluorouracil metabo­lism in mice with hepatic metastases.
      Eur. J. Cancer, 26: 1089-1092 (1990).
      


1940. Schols, D., De Clercq, E., Balzarini, J., Baba, M., Witvrouw, M., Hosoya, M., Andrei, G., Snoeck, R., Neyts, J., Pauwels, R., Nagy, M., Györgyi-Edelényi, J., Machovich, R., Horváth, I., Löw, M. & Görög, S.
      Sulphated polymers are potent and selective inhibitors of various enveloped viruses, including herpes simplex virus, cy­tomegalovirus, vesicular stomatitis virus, respiratory syncytial virus, and toga-, arena- and retroviruses.
      Antiviral Chem. Chemother., 1: 233-240 (1990).
      


1941. De Clercq, E.
      Therapeutic potential of phosphonylmethoxyalkylpurines and -pyrimidines as antiviral agents.
      Proceedings of the 9th International Symposium on Future Trends in Chemotherapy, Palexpo, Geneva, Switzerland, 26-28 March 1990.
      Drugs Exptl. Clin. Res., 16: 319-326 (1990).
      


1942. Balzarini, J. & De Clercq, E.
      9-ß-D-Arabinofuranosyladenine 5'-monophosphate (araAMP) is con­verted directly to its antivirally active 5'-triphosphate form by 5-phosphoribosyl-1-pyrophosphate (PRPP) synthetase.
      Biochem. Biophys. Res. Commun., 173: 781-787 (1990).
      


1943. De Clercq, E. & Andrei, G.M.
      Perspectivas en la quimioterapia contra la infección causada por el virus de la inmunode­ficiencia humana.
      Adelantos en Microbiologia y Enfermedades Infecciosas, 8: 29-44 (1990).
      


1944. Baba, M., E. De Clercq, S. Iida, H. Tanaka, I. Nitta, M. Ubasawa, H. Takashima, K. Sekiya, K. Umezu, H. Nakashima, S. Shigeta, R.T. Walker & T. Miyasaka.
      Anti-human immunodeficiency virus type 1 activities and pharmacokinetics of novel 6-substituted acyclouridine derivatives.
      Antimicrob. Agents Chemother., 34: 2358-2363 (1990).
      


1945. Van Aerschot, A., Everaert, D., Gosselin, G., Peeters, O., Bla­ton, N., De Ranter, C., Imbach, J.-L., Balzarini, J., De Clercq, E. & Herdewijn, P.
      2'-Azido-2',3'-dideoxythymidine: synthesis and crystal structure of a 2'-substituted dide­oxynucleoside.
      Antiviral Res., 14: 357-369 (1990).
      


1946. Molema, G., Jansen, R.W., Pauwels, R., De Clercq, E. & Meijer, D.K.F.
      Targeting of antiviral drugs to T4-lymphocytes. Anti-HIV activity of neoglycoprotein-AZTMP conjugates in vitro.
      Biochem. Pharmacol., 40: 2603-2610 (1990).
      


1947. Menage, M.J., De Clercq, E., Van Lierde, A., Easty, V.S., Darville, J.M., Cook, S.D. & Easty, D.L.
      Antiviral drug sensitivity in ocular herpes simplex virus infec­tion.
      Brit. J. Ophthalmol., 74: 532-535 (1990).
      


1948. Balzarini, J., Naesens, L., Robins, M.J. & De Clercq, E.
      Potentiating effect of ribavirin on the in vitro and in vivo antiretrovirus activities of 2',3'-dideoxyinosine and 2',3'-dideoxy-2,6-diaminopurine riboside.
      J. Acquir. Immun. Defic. Syndr., 3: 1140-1147 (1990).
      


1949. Ono, K., Nakane, H. & De Clercq, E.
      Potent inhibitory effects of the 5'-triphosphates of (E)-5-(2-bromovinyl)-2'-deoxyuridine and (E)-5-(2-bromovinyl)-1-ß-D-arabi­nofuranosyluracil on DNA polymerase .
      Eur. J. Biochem., 190: 463-467 (1990).
      


1950. Andrei, G. & De Clercq, E.
      Inhibitory effect of selected antiviral compounds on arenavirus replication in vitro.
      Antiviral Res., 14: 287-300 (1990).
      


1951. Cools, M. & De Clercq, E.
      Influence of S-adenosylhomocysteine hydrolase inhibitors on S-adenosylhomocysteine and S-adenosylmethionine pool levels in L929 cells.
      Biochem. Pharmacol.: 40, 2259-2264 (1990).
      


1952. Van Aerschot, A., Jie, L., Balzarini, J., De Clercq, E. & Herdewijn, P.
      5'-O-Phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
      The VIIIth Symposium on the Chemistry of Nucleic Acid Components, Bechyne Castle, Czechoslovakia, 17-21 September 1990.
      Collect. Czech. Chem. Commun., 55: 129-132 (1990).
      


1953. Dvoráková, H., Holý, A., Snoeck, R., Balzarini, J. & De Clercq, E.
      Acyclic nucleoside and nucleotide analogues derived from 1-deaza and 3-deazaadenine.
      The VIIIth Symposium on the Chemistry of Nucleic Acid Components, Bechyne Castle, Czechoslovakia, 17-21 September 1990.
      Collect. Czech. Chem. Commun., 55: 113-116 (1990).
      


1954. Mikhailopulo, I.A., Poopeiko, N.E., Pricota, T.I., Sivets, G.G., Balzarini, J. & De Clercq, E.
      Synthesis and biological properties of 2'-substituted 2',3'-dideoxy-3'-fluoro-D-ribonu­cleosides.
      The VIIIth Symposium on the Chemistry of Nucleic Acid Components, Bechyne Castle, Czechoslovakia, 17-21 September 1990.
      Collect. Czech. Chem. Commun., 55: 97-100 (1990).
      


1955. Tanaka, H., Baba, M., Ubasawa, M., Takashima, H., Sekiya, K., Miyasaka, T., Nitta, I., Walker, R.T. & De Clercq, E.
      The synthesis of novel 6-substituted acyclouridine derivatives which show specific inhibition of HIV-1.
      The VIIIth Symposium on the Chemistry of Nucleic Acid Components, Bechyne Castle, Czechoslovakia, 17-21 September 1990.
      Collect. Czech. Chem. Commun., 55: 89-92 (1990).
      


1956. Ali, Z., Qureshi, S., Shaw, G. & De Clercq, E.
      Anthracyclinones. Part 5. Synthesis of some anthracyclinones and 4-hydroxyanthracycli­nones containing a tertiary methyl carbinol function in ring A from D-glucose precursors.
      J. Chem. Soc. Perkin I: 2627-2636 (1990).
      


1957. Neyts, J., Snoeck, R., Schols, D., Balzarini, J. & De Clercq, E.
      Selective inhibition of human cytomegalovirus DNA synthesis by (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine [(S)-HPMPC] and 9-(1,3-dihydroxy-2-propoxyme­thyl)guanine (DHPG).
      Virology, 179: 41-50 (1990).
      


1958. Jie, L., Van Aerschot, A., Balzarini, J., Janssen, G., Busson, R., Hoogmartens, J., De Clercq, E. & Herdewijn, P.
      5'-O-Phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
      J. Med. Chem., 33: 2481-2487 (1990).
      


1959. Kumar, A., Coe, P.L., Jones, A.S., Walker, R.T., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of some cyclic phosphorami­date nucleoside deriva­tives.
      J. Med. Chem., 33: 2368-2375 (1990).
      


1960. Schols, D., Pauwels, R., Desmyter, J. & De Clercq, E.
      Flow cytometric method to monitor the destruction of CD4+ cells following their fusion with HIV-infected cells.
      Cytometry, 11: 736-743 (1990).
      


1961. Balzarini, J., Naesens, L. & De Clercq, E.
      Anti-retrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in vivo increases when it is less frequently administered.
      Int. J. Cancer, 46: 337-340 (1990).
      


1962. Szinai, I., Veres, Zs., Ganzler, K., Hegedus-Vajda, J. & De Clercq, E.
      In vitro and in vivo metabolism of the anti-herpes agent 5-(2-chloroethyl)-2'-de­oxyuridine.
      Proceedings of the Eighth International Bioanalytical Forum, Guildford, United King­dom, 5-8 September 1989, E. Reid & I.D. Wilson (eds.). Royal Society of Chemistry, Cambridge, pp. 219-220 (1990).
      


1963. Snoeck, R., Lagneaux, L., Delforge, A., Bron, D., Van der Auwera, P., Stryckmans, P., Balzarini, J. & De Clercq, E.
      Inhibitory effects of potent inhibitors of human immunodeficiency virus and cytomega­lovirus on the growth of human granulocyte-macrophage progenitor cells in vitro.
      Eur. J. Clin. Microbiol. Infect. Dis., 9: 615-619 (1990).
      


1964. Nakashima, H., Balzarini, J., Pauwels, R., Schols, D., Desmyter, J. & De Clercq, E.
      Anti-HIV-1 activity of antiviral compounds, as quantitated by a focal immunoassay in CD4+ HeLa cells and a plaque assay in MT-4 cells.
      J. Virol. Methods, 29: 197-208 (1990).
      


1965. De Clercq, E.
      Perspectives for the chemotherapy of AIDS.
      In "Animal Models in AIDS" (Proceedings of the International TNO Meeting on Animal Models in AIDS, Maastricht, The Netherlands, 23-26 October 1989), H. Schellekens & M.C. Horzinek (eds.).
      Elsevier Science Publishers B.V., Amsterdam, pp. 349-365 (1990).
      


1966. Rosenthal, S., Burkhardt, H., Rosenthal, H.A., Karge, E. & De Clercq, E.
      Bovine leukemia virus-infected sheep can serve as a model for the evaluation of antiretroviral compounds - the effect of treatment with suramin.
      In "Animal Models in AIDS" (Proceedings of the International TNO Meeting on Animal Models in AIDS, Maastricht, The Netherlands, 23-26 October 1989), H. Schellekens & M.C. Horzinek (eds.).
      Elsevier Science Publishers B.V., Amsterdam, pp. 265-273 (1990).
      


1967. Balzarini, J., Naesens, L., Slachmuylders, J., Niphuis, H., Rosenberg, I., Holý, A., Schellekens, H. & De Clercq, E.
      Potent anti-simian immunodeficiency virus (SIV) activity and pharmacokinetics of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in rhesus monkeys.
      In "Animal Models in AIDS" (Proceedings of the International TNO Meeting on Animal Models in AIDS, Maastricht, The Netherlands, 23-26 October 1989), H. Schellekens & M.C. Horzinek (eds.).
      Elsevier Science Publishers B.V., Amsterdam, pp. 131-138 (1990).
      


1968. Witvrouw, M., Baba, M., Balzarini, J., Pauwels, R. & De Clercq, E.
      Establishment of a bioassay to determine serum levels of dextran sulfate, a potent inhibi­tor of human immunodeficiency virus.
      In "Animal Models in AIDS" (Proceedings of the International TNO Meeting on Animal Models in AIDS, Maastricht, The Netherlands, 23-26 October 1989), H. Schellekens & M.C. Horzinek (eds.).
      Elsevier Science Publishers B.V., Amsterdam, pp. 97-102 (1990).
      


1969. De Clercq, E.
      The state of the art: chemotherapy of HIV infection.
      AIDS/HIV Experimental Treatment Directory of the American Foundation for AIDS Research 1990, 4: 5-11 (1990).
      


1970. De Clercq, E.
      Antivirale geneesmiddelen.
      In "Algemene Farmacotherapie" (zesde druk), red. H. Wesseling & C. Neef. Bohn Stafleu Van Loghum, Houten/Antwerpen, pp. 794-801 (1990).
      


1971. Puech, F., Gosselin, G., Balzarini, J., Good, S.S., Rideout, J.L., De Clercq, E. & Imbach, J.-L.
      Synthesis and biological evaluation of dinucleoside methylphos­phonates of 3'-azido-2',3'-dideoxythymidine and 2',3'-dideoxycytidine.
      Antiviral Res., 14: 11-24 (1990).
      


1972. Iigo, M., Miwa, M. & De Clercq, E.
      Optimal treatment regimens for 5'-deoxy-5-fluorouridine, with or without (E)-5-(2-bro­movinyl)-2'-deoxyuridine, against various tu­mors in mice.
      Jpn. J. Cancer Res. (Gann), 81: 431-435 (1990).
      


1973. Holý, A., Votruba, I., Merta, A., Cerny, J., Vesely, J., Vlach, J., Sediva, K., Rosenberg, I., Otmar, M., Hrebabecky, H., Travnicek, M., Vonka, V., Snoeck, R. & De Clercq, E.
      Acyclic nucleotide analogues: synthesis, antiviral activity and inhibitory effects on some cellular and virus-encoded enzymes in vitro.
      Antiviral Res., 13: 295-312 (1990).
      


1974. De Clercq, E., Bernaerts, R., Merta, A. & Rosenwirth, B.
      Mechanism of action of 5-(2-chloroethyl)-2'-deoxyuridine, a se­lective inhibitor of herpes simplex virus replication.
      Mol. Pharmacol., 37: 658-664 (1990).
      


1975. Yokota, T., Konno, K., Chonan, E., Mochizuki, S., Kojima, K., Shigeta, S. & De Clercq, E.
      Comparative activities of several nucleoside analogs against duck hepatitis B virus in vitro.
      Antimicrob. Agents Chemother., 34: 1326-1330 (1990).
      


1976. Egberink, H., Borst, M., Niphuis, H., Balzarini, J., Neu, H., Schellekens, H., De Clercq, E., Horzinek, M. & Koolen, M.
      Suppression of feline immunodeficiency virus infection in vivo by 9-(2-phos­phonomethoxyethyl)adenine.
      Proc. Natl. Acad. Sci. USA, 87: 3087-3091 (1990).
      


1977. Van Aerschot, A., Everaert, D., Balzarini, J., Augustyns, K., Jie, L., Janssen, G., Peeters, O., Blaton, N., De Ranter, C., De Clercq, E. & Herdewijn, P.
      Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyri­midine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides.
      J. Med. Chem., 33: 1833-1839 (1990).
      


1978. De Clercq, E.
      Selective virus inhibitors.
      Microbiologica, 13: 165-178 (1990).
      


1979. De Clercq, E.
      Perspectives for the chemotherapy of AIDS.
      Proceedings of the Fourth International Conference "To Live: Why", Pontificium Consi­lium de Apostolatu Pro Valetudinis Admi­nistris, Vatican City, 13-15 November 1989.
      Dolentium Hominum, Vol. 5, No. 13 "Vivre, Pourquoi ? Le SIDA", Vatican City, pp. 107-117 (1990).
      


1980. De Fazio, G., Alba, A.P.C., Vicente, M. & De Clercq, E.
      Antiviral activity of S-adenosylhomocysteine hydrolase inhibitors against plant viruses.
      Antiviral Res., 13: 219-226 (1990).
      


1981. Midoux, P., Negre, E., Roche, A.-C., Mayer, R., Monsigny, M., Balzarini, J., De Clercq, E., Mayer, E., Ghaffar, A. & Gangemi, J.D.
      Drug targeting: anti-HSV-1 activity of mannosylated polymer-bound 9-(2-phosphonyl­methoxyethyl)adenine.
      Biochem. Biophys. Res. Commun., 167: 1044-1049 (1990).
      


1982. Farrow, S.N., Jones, A.S., Kumar, A., Walker, R.T., Balzarini, J. & De Clercq, E.
      Synthesis and biological properties of novel phosphotriesters: a new approach to the introduction of biologically active nu­cleotides into cells.
      J. Med. Chem., 33: 1400-1406 (1990).
      


1983. Béres, J., Sagi, G., Tömösközi, I., Gruber, L., Baits-Gács, E., Ötvös, L. & De Clercq, E.
      Stereospecific synthesis and antiviral properties of different enantiomerically pure carbo­cyclic 2'-deoxyribonucleoside ana­logues derived from common chiral pools: (+)-(1R,5S)- and (-)-(1S,5R)-2-oxabicyclo[3.3.0]oct-6-en-3one.
      J. Med. Chem., 33: 1353-1360 (1990).
      


1984. Balzarini, J. & De Clercq, E.
      Acyclic and carbocyclic nucleoside analogues as inhibitors of HIV replication.
      In "Design of Anti-AIDS Drugs" (Pharmacochemistry Library vol. 14), E. De Clercq (ed.). Elsevier Science Publishers B.V., Amsterdam, Oxford, New York and Tokyo, pp. 175-194 (1990).
      


1985. Herdewijn, P. & De Clercq, E.
      Dideoxynucleoside analogues as inhibitors of HIV replication.
      In "Design of Anti-AIDS Drugs" (Pharmacochemistry Library vol. 14), E. De Clercq (ed.). Elsevier Science Publishers B.V., Amsterdam, Oxford, New York and Tokyo, pp. 141-174 (1990).
      


1986. Pauwels, R., Andries, K., Desmyter, J., Kukla, M.J., Heykants, J., De Clercq, E. & Jans­sen, P.A.J.
      Potent and selective inhibition of HIV-1 replication in vitro by a novel series of tetrahy­droimidazo-[4,5,1-jk][1,4]-benzodi­azepin-2(1H)-one and -thione (TIBO) derivatives.
      In "Design of Anti-AIDS Drugs" (Pharmacochemistry Library vol. 14), E. De Clercq (ed.). Elsevier Science Publishers B.V., Amsterdam, Oxford, New York and Tokyo, pp. 103-122 (1990).
      


1987. Baba, M. & De Clercq, E.
      Sulfated polymers as inhibitors of HIV replication.
      In "Design of Anti-AIDS Drugs" (Pharmacochemistry Library vol. 14), E. De Clercq (ed.). Elsevier Science Publishers B.V., Amsterdam, Oxford, New York and Tokyo, pp. 85-102 (1990).
      


1988. Schols, D. & De Clercq, E.
      HIV-CD4 interaction as target for anti-HIV agents.
      In "Design of Anti-AIDS Drugs" (Pharmacochemistry Library vol. 14), E. De Clercq (ed.). Elsevier Science Publishers B.V., Amsterdam, Oxford, New York and Tokyo, pp. 63-84 (1990).
      


1989. De Clercq, E.
      Perspectives for the chemotherapy of HIV infection: an introduction.
      In "Design of Anti-AIDS Drugs" (Pharmacochemistry Library vol. 14), E. De Clercq (ed.). Elsevier Science Publishers B.V., Amsterdam, Oxford, New York and Tokyo, pp. 1-24 (1990).
      


1990. Baba, M., Schols, D., De Clercq, E., Pauwels, R., Nagy, M., Györgyi-Edelényi, J., Löw, L. & Görög, S.
      Novel sulfated polymers as highly potent and selective inhibitors of human immunodefi­ciency virus (HIV) replication and giant cell formation.
      Antimicrob. Agents Chemother., 34: 134-138 (1990).
      


1991. De Clercq, E.
      Targets and strategies for the antiviral chemotherapy of AIDS.
      Trends in Pharmacological Sciences (TIPS), 11: 198-205 (1990).
      


1992. De Clercq, E.
      New acquisitions in the chemotherapy of viral infections.
      Verh. K. Acad. Geneeskd. Belg., 52: 69-99 (1990).
      


1993. Balzarini, J., Bernaerts, R., Verbruggen, A. & De Clercq, E.
      Role of the incorporation of (E)-5-(2-iodovinyl)-2'-deoxyuridine and its carbocyclic ana­logue into DNA of herpes simplex virus type 1-infected cells in the antiviral effects of these com­pounds.
      Mol. Pharmacol., 37: 402-407 (1990).
      


1994. Balzarini, J., De Clercq, E., Baumgartner, H., Bodenteich, M. & Griengl, H.
      Carbocyclic 5-iodo-2'-deoxyuridine (C-IDU) and carbocyclic (E)-5-(2-bromovinyl)-2'-deoxyuridine (C-BVDU) as unique examples of chiral molecules where the two enan­tiomeric forms are biologi­cally active: interaction of the (+)- and (-)-enantiomers of C-IDU and C-BVDU with the thymidine kinase of herpes simplex virus type 1.
      Mol. Pharmacol., 37: 395-401 (1990).
      


1995. Balzarini, J., Sobis, H., Naesens, L., Vandeputte, M. & De Clercq, E.
      Inhibitory effects of 9-(2-phosphonylmethoxyethyl)adenine and 3'-azido-2',3'-dide­oxythymidine on tumor development in mice inocu­lated intracerebrally with Moloney murine sarcoma virus.
      Int. J. Cancer, 45: 486-489 (1990).
      


1996. De Clercq, E.
      New developments in anti-AIDS drugs.
      Proceedings of the 7th Noordwijkerhout-Camerino Symposium, Noord­wijkerhout, The Netherlands, 5-8 September 1989.
      In "Trends in Drug Research", V. Claassen (ed.). Elsevier Science Publishers B.V., Amsterdam, pp. 133-152 (1990).
      


1997. Schols, D., Pauwels, R., Desmyter, J. & De Clercq, E.
      Dextran sulfate and other polyanionic anti-HIV compounds specifi­cally interact with the viral gp120 glycoprotein expressed by T-cells persistently infected with HIV-1.
      Virology, 175: 556-561 (1990).
      


1998. Baba, M., Schols, D., Pauwels, R., Nakashima, H. & De Clercq, E.
      Sulfated polysaccharides as potent inhibitors of HIV-induced syn­cytium formation: a new strategy towards AIDS chemotherapy.
      J. Acquir. Immun. Defic. Syndr., 3: 493-499 (1990).
      


1999. Iigo, M., Nishikata, K.-i., Nakajima, Y., Szinai, I., Veres, Z., Szabolcs, A. & De Clercq, E.
      Differential effects of 2,2'-anhydro-5-ethyluridine, a uridine phosphorylase inhibitor, on the antitumor activity of 5-fluo­rouridine and 5-fluoro-2'-deoxyuridine.
      Biochem. Pharmacol., 39: 1247-1253 (1990).
      


2000. Witvrouw, M., Baba, M., Balzarini, J., Pauwels, R. & De Clercq, E.
      Establishment of a bioassay to determine serum levels of dextran sulfate and pentosan polysulfate, two potent inhibitors of human immunodeficiency virus.
      J. Acquir. Immun. Defic. Syndr., 3: 343-347 (1990).
      


2001. Kumar, A., Lewis, M., Shimizu, S.-I., Walker, R.T., Snoeck, R. & De Clercq, E.
      E-5-(2-Chlorovinyl)-2'-deoxycytidine: synthesis and antiherpetic activity.
      Antiviral Chemistry & Chemotherapy, 1: 35-40 (1990).
      


2002. Aduma, P.J., Gupta, S.V. & De Clercq, E.
      Antiherpes virus activity and effect on deoxyribonucleoside triphosphate pools of (E)-5-(2-bromovinyl)-2'-deoxycytidine in combination with deaminase inhibitors.
      Antiviral Res., 13: 111-126 (1990).
      


2003. Baba, M., De Clercq, E., Schols, D., Pauwels, R., Snoeck, R., Van Boeckel, C., Van Dedem, G., Kraaijeveld, N., Hobbelen, P., Otten­heijm, H. & den Hollander, F.
      Novel sulfated polysaccharides: dissociation of anti-human im­munodeficiency virus activity from antithrombin activity.
      J. Infect. Dis., 161: 208-213 (1990).
      


2004. Ito, M., Baba, M., Mori, S., Hirabayashi, K., Sato, A., Shigeta, S. & De Clercq, E.
      Tumor necrosis factor antagonizes inhibitory effect of azi­dothymidine on human immu­nodeficiency virus (HIV) replication in vitro.
      Biochem. Biophys. Res. Commun., 166: 1095-1101 (1990).
      


2005. Wigerinck, P., Van Aerschot, A., Janssen, G., Claes, P., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis and antiviral activity of 3'-heterocyclic substituted 2',3'-dideoxythymidines.
      J. Med. Chem., 33: 868-873 (1990).
      


2006. Hiebl, J., Zbiral, E., Balzarini, J. & De Clercq, E.
      Synthesis, antiretrovirus effects, and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine.
      J. Med. Chem., 33: 845-848 (1990).
      


2007. Pauwels, R., Andries, K., Desmyter, J., Schols, D., Kukla, M.J., Breslin, H.J., Raey­maeckers, A., Van Gelder, J., Woestenborghs, R., Heykants, J., Schellekens, K., Janssen, M.A.C., De Clercq E. & Janssen, P.A.J.
      Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives.
      Nature, 343: 470-474 (1990).
      


2008. De Clercq, E., Bernaerts, R., Shealy, Y.F. & Montgomery, J.A.
      Broad-spectrum antiviral activity of carbodine, the carbocyclic analogue of cytidine.
      Biochem. Pharmacol., 39: 319-325 (1990).
      


2009. Cools, M., Hasobe, M., De Clercq, E. & Borchardt, R.T.
      Mechanism of the synergistic antiviral and cytostatic activity of (RS)-3-(adenin-9-yl)-2-hydroxypropanoic acid isobutyl ester and D,L-homocysteine.
      Biochem. Pharmacol., 39: 195-202 (1990).
      



86 publications in the year 1989



2010. Herdewijn, P., Van Aerschot, A., Balzarini, J. & De Clercq, E.
      2',3'-Dideoxynucleoside analogues as inhibitors of human immuno­deficiency virus.
      In: "New Methods in Drug Research", Vol. 3, A. Makriyannis (ed.).
      J.R. Prous Science Publishers, Barcelona, pp. 103-122 (1989).
      


2011. Wigerinck, P., Van Aerschot, A., Claes, P., Balzarini, J., De Clercq, E. & Herdewijn, P.
      3'-(1,2,3-Triazol-1-yl)-2',3'-dideoxythymidine and 3'-(1,2,3-tri­azol-1-yl)-2',3'-dideoxy­uridine.
      J. Heterocyclic Chem., 26: 1635-1642 (1989).
      


2012. Lesiak, K., De Clercq, E. & Torrence, P.F.
      Adducts of mannose 6-phosphate with 5-iodo-2'-deoxyuridine and 2-5A as potential antiviral agents.
      Nucleosides & Nucleotides, 8: 1387-1398 (1989).
      


2013. Ward, S.G., Taylor, R.C., Köpf-Maier, P., Köpf, H., Balzarini, J. & De Clercq, E.
      Assessment of the in vitro broad-spectrum antiviral activity of some selected antitumor metallocene and metallocenium complexes.
      Applied Organometallic Chemistry, 3: 491-497 (1989).
      


2014. Balzarini, J., Matthes, E., Meeus, P., Johns, D.G. & De Clercq, E.
      The antiretroviral and cytostatic activity, and metabolism of 3'-azido-2',3'-dide­oxythymidine, 3'-fluoro-2',3'-dideoxythymi­dine and 2',3'-dideoxycytidine are highly cell type-dependent.
      Proceedings of the Sixth International Symposium on Human Purine & Pyrimidine Metabolism, Hakone, Japan, 17-21 July 1988.
      In: "Purine and Pyrimidine Metabolism in Man VI", part B, K. Mikanagi, K. Nishioka & W.N. Kelley (eds.).
      Plenum Publishing Corporation, New York, pp. 407-413 (1989).
      


2015. Baba, M., Tanaka, H., De Clercq, E., Pauwels, R., Balzarini, J., Schols, D., Nakashima, H., Perno, C.-F., Walker, R.T. & Miyasaka, T.
      Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substi­tuted acyclouridine derivative.
      Biochem. Biophys. Res. Commun., 165: 1375-1381 (1989).
      


2016. De Clercq, E.
      Chemotherapy of viral infections in immunocompromised patients.
      Proceedings of the IVth Symposium on Clinical Microbiology, Monte Porzio Catone, Italy, 30 March-1 April 1989.
      In "Microbiological, Chemotherapeutical and Immunolo­gical Problems in High Risk Patients", E. Garaci, G. Renzini, F. Filadoro, A.L. Goldstein & J. Verhoef (eds.). Serono Symposia Publications, Raven Press, New York, pp. 231-241 (1989).
      


2017. Szinai, I. & De Clercq, E.
      Biotransformation of 5-(2-chloroethyl)-2'-deoxyuridine in male NMRI mice.
      Drug Metabolism and Disposition, 17: 683-689 (1989).
      


2018. Naesens, L., Balzarini, J. & De Clercq, E.
      Antiretroviral activity and pharmacokinetics of 9-(2-phosphonylmethoxyethyl)adenine in mice.
      In "Recent Advances in Chemotherapy" (Proceedings of the 16th International Congress of Chemotherapy, Jerusalem, Israel, 11-16 June 1989), E. Rubinstein and D. Adam (eds).
      E. Lewin-Epstein Ltd., Offset Printers, Jerusalem, Israel, pp. 467.1-467.2 (1989).
      


2019. Nakashima, H., Pauwels, R., Baba, M., Schols, D., Desmyter, J. & De Clercq, E.
      Tetrazolium-based plaque assay for HIV-1 and HIV-2, and its use in the evaluation of antiviral compounds.
      J. Virol. Methods, 26: 319-330 (1989).
      


2020. Schols, D., Snoeck, R., Neyts, J. & De Clercq, E.
      Detection of immediate early, early and late antigens of human cytomegalovirus by flow cytometry.
      J. Virol. Methods, 26: 247-254 (1989).
      


2021. Herdewijn, P., Charubala, R., De Clercq, E. & Pfleiderer, W.
      Nucleotides. Part XXXII. Synthesis of 2'-5' connected oligonu­cleotides. Prodrugs for antiviral and antitumoral nucleosides.
      Helvetica Chimica Acta, 72: 1739-1748 (1989).
      


2022. Ward, S.G., Taylor, R.C., Crowe, A.J., Balzarini, J. & De Clercq, E.
      Assessment of the in vitro broad-spectrum antiviral activity of some selected antitumor organotin complexes.
      Applied Organometallic Chemistry, 3: 431-436 (1989).
      


2023. Naesens, L., Balzarini, J., Rosenberg, I., Holý, A. & De Clercq, E.
      9-(2-Phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP): a novel agent with anti-human immunodeficiency virus activity in vitro and potent anti-Moloney murine sarcoma virus activity in vivo.
      Eur. J. Clin. Microb. & Infect. Dis., 8: 1043-1047 (1989).
      


2024. Balzarini, J., Van Aerschot, A., Herdewijn, P. & De Clercq, E.
      2',3'-Didehydro-2',3'-dideoxy-5-chlorocytidine is a selective anti-retrovirus agent.
      Biochem. Biophys. Res. Commun., 164: 1190-1197 (1989).
      


2025. Burkhardt, H., Rosenthal, S., Rosenthal, H.-A., Karge, E. & De Clercq, E.
      Treatment of bovine leukaemia virus-infected sheep with suramin: an animal model for the development of antiretroviral com­pounds.
      Acta Virol., 33: 305-313 (1989).
      


2026. Mul, Y.M., van Miltenburg, R.T., De Clercq, E. & van der Vliet, P.C.
      Mechanism of inhibition of adenovirus DNA replication by the acyclic nucleoside triphosphate analogue (S)-HPMPApp: influence of the adenovirus DNA binding protein.
      Nucleic Acids Res., 17: 8917-8929 (1989).
      


2027. Miyasaka, T., Tanaka, H., Baba, M., Hayakawa, H., Walker, R.T., Balzarini, J. & De Clercq, E.
      A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine.
      J. Med. Chem., 32: 2507-2509 (1989).
      


2028. De Clercq, E.
      Development of new anti-HIV agents and elucidation of their me­chanism of action.
      In "AIDS 89-90: News and Views on Research and Control", G. de-Thé (ed.). McGraw-Hill, Paris, pp. 191-197 (1989).
      


2029. Gangemi, J.D., Cozens, R.M., De Clercq, E., Balzarini, J. & Hochkeppel, H.-K.
      9-(2-Phosphonylmethoxyethyl)adenine in the treatment of murine acquired immunodefi­ciency disease and opportunis­tic herpes sim­plex virus infections.
      Antimicrob. Agents Chemother., 33: 1864-1868 (1989).
      


2030. Bijlenga, G., Joubert, L. & De Clercq E.
      Isolement et caractères in vitro et in vivo d'un clone de virus sauvage de la maladie d'Aujeszky résistant à la bromovinyl­désoxyuridine.
      Ann. Rech. Vét., 20: 259-267 (1989).
      


2031. Hasobe, M., McKee, J.G., Ishii, H., Cools, M., Borchardt, R.T. & De Clercq, E.
      Elucidation of the mechanism by which homocysteine potentiates the anti-vaccinia virus effects of the S-adenosylhomocysteine hydro­lase inhibitor 9-(trans-2',trans-3'-dihy­droxycyclopent-4'-enyl)-adenine.
      Mol. Pharmacol., 36: 490-496 (1989).
      


2032. De Clercq, E.
      Inhibition of the replication of DNA viruses by phosphonyl­methoxyalkylpurines and-pyrimidines.
      In "Proceedings of the VIth Mediterranean Congress of Chemothe­rapy", Taormina - Giardini Naxos, Italy, 22-27 May 1988.
      J. Chemother., Suppl. 4: 1074-1076 (1989).
      


2033. Van Aerschot, A., Herdewijn, P., Janssen, G., Cools, M. & De Clercq, E.
      Synthesis and antiviral activity evaluation of 3'-fluoro-3'-de­oxyribonucleosides: broad-spectrum antiviral activity of 3'-fluoro-3'-deoxyadenosine.
      Antiviral Res., 12: 133-150 (1989).
      


2034. Lown, J.W., Krowicki, K., Balzarini, J., Newman, R.A. & De Clercq, E.
      Novel linked antiviral and antitumor agents related to netropsin and distamycin: synthesis and biological evaluation.
      J. Med. Chem., 32: 2368-2375 (1989).
      


2035. Hosoya, M., Shigeta, S. & De Clercq, E.
      Inhibitory effect of selected antiviral compounds on measles (SSPE) virus replication in vitro.
      Antiviral Research, 12: 87-98 (1989).
      


2036. Van Bijsterveld, O.P., Meurs, P.J., De Clercq, E. & Maudgal, P.C.
      Bromovinyldeoxyuridine and interferon treatment in ulcerative herpetic keratitis: a double masked study.
      Brit. J. Ophthalmol., 73: 604-607 (1989).
      


2037. Schols, D., Pauwels, R., Baba, M., Desmyter, J. & De Clercq, E.
      Syncytium formation and destruction of bystander CD4+ cells co­cultured with T cells persistently infected with human immunode­ficiency virus as demonstrated by flow cytometry.
      J. Gen. Virol., 70: 2397-2408 (1989).
      


2038. Smith, M.S., Brian, E.L., De Clercq, E. & Pagano, J.S.
      Susceptibility of human immunodeficiency virus type 1 replication in vitro to acyclic adenosine analogs and synergy of the analogs with 3'-azido-3'-deoxythymidine.
      Antimicrob. Agents Chemother., 33: 1482-1486 (1989).
      


2039. Herdewijn, P., Balzarini, J., Pauwels, R., Janssen, G., Van Aer­schot, A. & De Clercq, E.
      Synthesis and biological activity of the mono- and diamino ana­logues of 2'-deoxy­adenosine, cordycepin, 9-(3-deoxy-ß-D-threo-pentofuranosyl)adenine (a structural com­ponent of agrocin 84) and 9-(2-deoxy-ß-D-threo-pentofuranosyl)adenine.
      Nucleosides & Nucleotides, 8: 1231-1257 (1989).
      


2040. Van Aerschot, A., Balzarini, J., Pauwels, R., Wigerinck, P., De Clercq, E. & Herdewijn, P.
      Sugar- and base-modified 2',3'-dideoxynucleosides as potential anti-AIDS drugs.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 1125-1126 (1989).
      


2041. Van Aerschot, A., Balzarini, J., De Clercq, E. & Herdewijn, P.
      Synthesis of 3'-fluoro-3'-deoxyribonucleosides: anti-HIV-1 and cytostatic properties.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 1123-1124 (1989).
      


2042. Van Aerschot, A., Balzarini, J., Pauwels, R., Kerremans, L., De Clercq, E. & Herdewijn, P.
      Influence of fluorination of the sugar moiety on the anti-HIV-1 activity of 2',3'-dide­oxynucleosides.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 1121-1122 (1989).
      


2043. Pauwels, R., Debyser, Z., Balzarini, J., Baba, M., Desmyter, J., Rayner, B., Morvan, F., Imbach, J.L. & De Clercq, E.
      Alpha-oligodeoxynucleotides as inhibitors of HIV reverse transcriptase.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 995-1000 (1989).
      


2044. Alderweireldt, F.C., Vrijens, I., Esmans, E.L., Wotring, L.L., Townsend, L.B., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of 2-carbamoyl-5-D-ribofuranosylpyridine.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 891-894 (1989).
      


2045. Balzarini, J., Baumgartner, H., Bodenteich, M., De Clercq, E. & Griengl, H.
      Synthesis and biological properties of (+)- and (-)-(E)-5-(2-bro­movinyl)-2'-deoxy-1'a-carbauridine.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 855-858 (1989).
      


2046. Camarasa, M.-J., Díaz-Ortíz, A., Calvo-Mateo, A., De las Heras, F.G., Balzarini, J. & De Clercq, E.
      Synthesis and evaluation of antiviral activity of 3'-C-cyano-3'-deoxynucleosides.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Ap­plications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 837-840 (1989).
      


2047. De Clercq, E., Van Aerschot, A., Herdewijn, P., Baba, M., Pauwels, R. & Balzarini, J.
      Anti-HIV-1 activity of 2',3'-dideoxynucleoside analogues: struc­ture-activity relationship.
      Proceedings of the "Eighth International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Orange Beach, Alabama, USA, 2-5 October 1988.
      Nucleosides & Nucleotides, 8: 659-671 (1989).
      


2048. De Clercq, E.
      New acquisitions in the development of anti-HIV agents.
      Antiviral Res., 12: 1-20 (1989).
      


2049. De Clercq, E., Cools, M., Balzarini, J., Marquez, V.E., Borcherding, D.R., Bor­chardt, R.T., Drach, J.C., Kitaoka, S. & Konno, T.
      Broad-spectrum antiviral activities of neplanocin A, 3-deazaneplanocin A, and their 5'-nor derivatives.
      Antimicrob. Agents Chemother., 33: 1291-1297 (1989).
      


2050. Balzarini, J., Baumgartner, H., Bodenteich, M., De Clercq, E. & Griengl, H.
      Synthesis and antiviral activity of the enantiomeric forms of carba-5-iodo-2'-de­oxyuridine and carba-(E)-5-(2-bromovinyl)-2'-deoxyuridine.
      J. Med. Chem., 32: 1861-1865 (1989).
      


2051. Robins, M.J., Wood, S.G., Dalley, N.K., Herdewijn, P., Balzarini, J. & De Clercq, E.
      Nucleic acid related compounds. 57. Synthesis, X-ray crystal structure, lipophilic parti­tion properties, and antiretroviral ac­tivities of anomeric 3'-azido-2',3'-dideoxy-2,6-diaminopurine ri­bosides.
      J. Med. Chem., 32: 1763-1768 (1989).
      


2052. Van Aerschot, A., Herdewijn, P., Balzarini, J., Pauwels, R. & De Clercq, E.
      3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.
      J. Med. Chem., 32: 1743-1749 (1989).
      


2053. Camarasa, M.-J., Diaz-Ortiz, A., Calvo-Mateo, A., De Las Heras, F.G., Balzarini, J. & De Clercq, E.
      Synthesis and antiviral activity of 3'-C-cyano-3'-deoxynucleosides.
      J. Med. Chem., 32: 1732-1738 (1989).
      


2054. De Clercq, E.
      Perspectives for the chemotherapy of HIV infection.
      American Foundation for AIDS Research, AIDS/HIV Experimental Treatment Directory, 3: 21-28 (1989).
      


2055. De Clercq, E.
      New promising inhibitors of the human immunodeficiency virus.
      In "Current Opinion in Infectious Diseases" (Section Editor: E. De Clercq). Vol. 2, pp. 401-410 (1989).
      


2056. De Clercq, E.
      Antimicrobial agents: viral. Overview.
      In "Current Opinion in Infectious Diseases" (Section Editor: E. De Clercq). Vol. 2, pp. 383-385 (1989).
      


2057. Nakashima, H., Yoshida, O., Baba, M., De Clercq, E. & Yamamoto, N.
      Anti-HIV activity of dextran sulphate as determined under dif­ferent experimental condi­tions.
      Antiviral Res., 11: 233-246 (1989).
      


2058. Ono, K., Nakane, H., Herdewijn, P., Balzarini, J. & De Clercq, E.
      Differential inhibitory effects of several pyrimi­dine 2',3'-dideoxynucleoside 5'-triphos­phates on the activities of reverse transcriptase and various cel­lular DNA polymerases.
      Mol. Pharmacol., 35: 578-583 (1989).
      


2059. Balzarini, J., Van Aerschot, A., Pauwels, R., Baba, M., Schols, D., Herdewijn, P. & De Clercq, E.
      5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of hu­man immunodeficiency virus (HIV): potent and selective anti-HIV ac­tivity of 3'-fluoro-2',3'-dideoxy-5-chlo­rouridine.
      Mol. Pharmacol., 35: 571-577 (1989).
      


2060. De Clercq, E.
      Viral DNA synthesis as target for the antiviral action of nu­cleoside analogues.
      In "Antiviral Drugs, Basic and Therapeutic Aspects" (Proceedings of the International Symposium on "Basic and Thera­peutic Aspects of Antiviral Drugs", Copanello (Catanzaro), Italy, 17-19 Septem­ber 1987), R. Caliò & G. Nisticò (eds.).
      Pythagora Press, Rome-Milan, Italy, pp. 47-72 (1989).
      


2061. Balzarini, J., Herdewijn, P. & De Clercq, E.
      Differential patterns of intracellular metabolism of 2',3'-dide­hydro-2',3'-dideoxy­thymidine and 3'-azido-2',3'-dideoxythymi­dine, two potent anti-human immunode­fi­ciency virus compounds.
      J. Biol. Chem., 264: 6127-6133 (1989).
      


2062. Balzarini, J., Herdewijn, P. & De Clercq, E.
      Potentiating effect of ribavirin on the anti-retrovirus activity of 3'-azido-2,6-diaminopu­rine-2',3'-dideoxyriboside in vitro and in vivo.
      Antiviral Res., 11: 161-172 (1989).
      


2063. Balzarini, J. & De Clercq, E.
      Inhibitory effects of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and related com­pounds on herpes simplex virus (HSV)-in­fected cells and HSV thymidine kinase gene-transformed cells.
      Meth. and Find. Exp. Clin. Pharmacol., 11: 379-389 (1989).
      


2064. Baba, M., Schols, D., Nakashima, H., Pauwels, R., Parmentier, G., Meijer, D.K.F. & De Clercq, E.
      Selective activity of several cholic acid derivatives against hu­man immunodeficiency virus replication in vitro.
      J. Acquir. Immun. Defic. Syndr., 2: 264-271 (1989).
      


2065. Bernaerts, R., Desgranges, C. & De Clercq, E.
      (E)-5-(2-Bromovinyl)uridine requires phosphorylation by the her­pes simplex virus (type 1)-induced thymidine kinase to ex­press its antiviral activity.
      Biochem. Pharmacol., 38: 1955-1961 (1989).
      


2066. Iigo, M., Nishikata, K.-i., Nakajima, Y., Hoshi, A., Okudaira, N., Odagiri, H. & De Clercq, E.
      Enhancing effect of bromovinyldeoxyuridine on anti­tumor activity of 5'-deoxy-5-fluo­rouridine against adenocarcinoma 755 in mice. Correlation with pharma­cokinetics of plasma 5-fluorouracil le­vels.
      Biochem. Pharmacol., 38: 1885-1889 (1989).
      


2067. De Clercq, E., Cools, M. & Balzarini, J.
      Homocysteine potentiates the antiviral and cytostatic activity of those nucleoside ana­logues that are targeted at S-adenosyl­homocysteine hydrolase.
      Biochem. Pharmacol., 38: 1771-1778 (1989).
      


2068. Schols, D., Baba, M., Pauwels, R., Desmyter, J. & De Clercq, E.
      Specific interaction of aurintricarboxylic acid with the human immunodeficiency virus/CD4 cell receptor.
      Proc. Natl. Acad. Sci. USA, 86: 3322-3326 (1989).
      


2069. Ayisi, N.K., Sacks, S.L., De Clercq, E. & Carton, H.
      Pharmacokinetic behavior of bromovinyldeoxyuridine in herpes en­cephalitis patients.
      Int. J. Exp. Clin. Chemother., 2: 27-38 (1989).
      


2070. Baba, M., Pauwels, R., Balzarini, J., Schols, D. & De Clercq, E.
      Coumermycin A1 is a potent inhibitor of human immunodeficiency virus (HIV) replica­tion in vitro.
      Int. J. Exp. Clin. Chemother., 2: 15-20 (1989).
      


2071. Debart, F., Perigaud, C., Gosselin, G., Mrani, D., Rayner, B., Le Ber, P., Auclair, C., Balzarini, J., De Clercq, E., Pao­letti, C. & Imbach, J.-L.
      Synthesis, DNA binding and biological evaluation of synthetic precursors and novel analogues of netropsin.
      J. Med. Chem., 32: 1074-1083 (1989).
      


2072. Belmans, M., Vrijens, I., Esmans, E.L., Dommisse, R.A., Le­poivre, J.A., Alderweireldt, F.C., Townsend, L.B., Wotring, L.L., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of a series of substituted pyridine-C-nucleosides. Part V: 3-Chloro-4-(D-ribofuranosyl)-pyridine and 3-(D-ribofuranosyl)-2-pyridone.
      Nucleosides & Nucleotides, 8: 307-315 (1989).
      


2073. De Clercq, E.
      Activity of sulfated polysaccharides against the human immuno­deficiency virus.
      Proceedings of the Xth International Symposium on Medici­nal Chemistry, Budapest, Hungary, 15-19 August 1988.
      In: "Trends in Medicinal Chemistry '88", H. van der Goot, G. Domány, L. Pallos and H. Timmerman (eds.).
      Elsevier Science Publishers B.V., Amsterdam, The Netherlands, pp. 729-742 (1989).
      


2074. De Clercq, E.
      Molecular targets of chemotherapeutic agents against the human immunodeficiency virus.
      Proceedings of the Bayer AG Centenary Symposium on Perspectives in Antiinfective Therapy, Washington DC, USA, 31 August-3 Septem­ber 1988.
      In: "Perspectives in Antiinfective Therapy", G.G. Jackson, H.D. Schlumberger and H.J. Zeiler (eds).
      Current Topics in Infectious Diseases, 2: 255-267 (1989).
      


2075. Bobek, M., An, S.-H., Skrincosky, D., De Clercq, E. & Bernacki, R.J.
      2'-Fluorinated isonucleosides. 1. Synthesis and bio­logical acti­vity of some methyl 2'-deoxy-2'-fluoro-2'-pyrimidinyl-D-ara­binopyranosides.
      J. Med. Chem., 32: 799-807 (1989).
      


2076. Balzarini, J. & De Clercq, E.
      The antiviral activity of 9-ß-D-arabinofuranosyladenine is en­hanced by the 2',3'-dide­oxyriboside, the 2',3'-didehydro-2',3'-dideoxyriboside and the 3'-azido-2',3'-dideoxyri­boside of 2,6-di­aminopurine.
      Biochem. Biophys. Res. Commun., 159: 61-67 (1989).
      


2077. Cools, M. & De Clercq, E.
      Correlation between the antiviral activity of acyclic and car­bocyclic adenosine ana­logues in murine L929 cells and their in­hibitory effect on L929 cell S-adenosylhomocys­teine hydrolase.
      Biochem. Pharmacol., 38: 1061-1067 (1989).
      


2078. Balzarini, J., Cools, M. & De Clercq, E.
      Estimation of the lipophilicity of anti-HIV nucleo­side analogues by determination of the partition co­efficient and retention time on a lichrospher 60 RP-8 HPLC column.
      Biochem. Biophys. Res. Commun., 158: 413-422 (1989).
      


2079. Balzarini, J., Van Aerschot, A., Herdewijn, P. & De Clercq, E.
      5-Chloro-substituted derivatives of 2',3'-didehydro-2',3'-dideoxyuridine, 3'-fluoro-2',3'-dideoxyuridine and 3'-azido-2',3'-dideoxyuridine as anti-HIV agents.
      Biochem. Pharmacol., 38: 869-874 (1989).
      


2080. Ito, M., Baba, M., Hirabayashi, K., Matsumoto, T., Suzuki, M., Suzuki, S., Shigeta, S. & De Clercq, E.
      In vitro activity of mannan sulfate, a novel sulfated polysaccha­ride, against human immunodeficiency virus type 1 and other en­veloped viruses.
      Eur. J. Clin. Microbiol. Infect. Dis., 8: 171-173 (1989).
      


2081. De Clercq, E.
      Antiviral activity of new nucleoside and nucleotide analogues.
      In "Highlights of Modern Biochemistry (Proceedings of the 14th International Congress of Bioche­mistry", Prague, Czechoslovakia, 10-15 July 1988), A. Kotyk, J. Skoda, V. Paces & V. Kostka (eds.). VSP International Science Publishers, Zeist, The Nether­lands, pp. 1527-1537 (1989).
      


2082. Schols, D., Baba, M., Pauwels, R. & De Clercq, E.
      Flow cytometric method to demonstrate whether anti-HIV-1 agents inhibit virion binding to T4+ cells.
      J. Acquir. Immun. Defic. Syndr., 2: 10-15 (1989).
      


2083. Ito, M., Baba, M., Sato, A., Hirabayashi, K., Ta­nabe, F., Shigeta, S. & De Clercq, E.
      Tumor necrosis factor enhances replication of human immunodefi­ciency virus (HIV) in vitro.
      Biochem. Biophys. Res. Commun., 158: 307-312 (1989).
      


2084. De Clercq, E., Holý, A. & Rosenberg, I.
      Efficacy of phosphonylmethoxyalkyl derivatives of adenine in ex­perimental herpes simplex virus and vaccinia virus infections in vivo.
      Antimicrob. Agents Chemother., 33: 185-191 (1989).
      


2085. De Clercq, E.
      Potential drugs for the treatment of AIDS.
      J. Antimicrob. Chemother., 23 (Suppl. A): 35-46 (1989).
      


2086. Balzarini, J., Naesens, L., Herdewijn, P., Rosenberg, I., Holý, A., Pauwels, R., Baba, M., Johns, D.G. & De Clercq, E.
      Marked in vivo antiretrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine, a selec­tive anti-human immunodeficiency virus agent.
      Proc. Natl. Acad. Sci. USA, 86: 332-336 (1989).
      


2087. De Clercq, E.
      Therapeutische benadering van virusinfecties: Rol van S-adeno­sylhomocysteine hydro­lase als doelwitenzym.
      Tijdschr. Geneesk., 45: 93-98 (1989).
      


2088. Baraldi, P.G., Guarneri, M., Manfredini, S., Simoni, D., Balzarini, J. & De Clercq, E.
      Synthesis and cytostatic activity of geiparvarin analogues.
      J. Med. Chem., 32: 284-288 (1989).
      


2089. Béres, J., Bentrude, W.G., Ötvös, L., Balzarini, J. & De Clercq, E.
      Synthesis and cytostatic and antiviral activities of 1-ß-D-ri­bofuranosyl-5-alkylcytosine (5-alkylcytidine)cyclic 3',5'-mono-phosphates.
      J. Med. Chem., 32: 224-228 (1989).
      


2090. De Clercq, E.
      Antiviral agents: facts and prospects.
      In: "Recent Advances in Infection", Number Three, D.S. Reeves & A.M. Ged­des (eds.).
      Churchill Livingstone, Edinburgh, London, Melbourne and New York, pp. 45-61 (1989).
      


2091. Hamoir, G., Sonveaux, E., Iigo, M. & De Clercq, E.
      The cyclic dimer of 5-fluoro-2'-deoxyuridylic acid: a potent an­ticancer agent.
      Nucleosides & Nucleotides, 8, 285-295 (1989).
      


2092. Kaul, R., Hempel, B. & De Clercq, E.
      Penetration und Wirksamkeit von Edoxudin in vitro und in vivo.
      Arzneimittel-Forschung/Drug Research, 39: 366-368 (1989).
      


2093. Baba, M., Pauwels, R., Balzarini, J., Desmyter, J. & De Clercq, E.
      Antiviral activity of heparin and dextran sulfate against human immunodeficiency virus (HIV) in vitro.
      Ann. N.Y. Acad. Sci., 556: 419-421 (1989).
      


2094. Holý, A., De Clercq, E. & Votruba, I.
      Phosphonylmethyl ethers of nucleosides and their acyclic analogs.
      In "Nucleotide Analogues as Antiviral Agents" (Proceedings of Symposium on Nucleo­side Analogues as Antiviral Agents, 196th National Meeting of the ACS (American Chemical Society), Los Angeles, Califor­nia, USA, 25-30 September 1988), J.C. Martin (ed.).
      American Chemical Society, Washington D.C., pp. 51-71 (1989).
      


2095. Ameye, C., Sundmacher, R. & De Clercq, E.
      Topical BVDU plus low-dosage steroids in the treatment of chronic relapsing zoster keratouveitis. A pilot study.
      Graefe's Arch. Clin. Exp. Ophthalmol., 227: 118-122 (1989).
      



52 publications in the year 1988



2096. Ito, M., Sato, A., Hirabayashi, K., Tanabe, F., Shigeta, S., Baba, M., De Clercq, E., Naka­shima, H. & Yamamoto, N.
      Mechanism of inhibitory effect of glycyrrhizin on replication of human immunodefi­ciency virus (HIV).
      Antiviral Res., 10: 289-298 (1988).
      


2097. De Clercq, E.
      Perspectives for the chemotherapy of AIDS.
      Chemioterapia, 7: 357-364 (1988).
      


2098. Balzarini, J. & De Clercq, E.
      Differential mechanism of inhibitory action of (E)-5-(2-bro­movinyl)-2'-deoxyuridine (BVDU) and related compounds in herpes simplex virus (HSV)-infected cells versus HSV thymidine kinase gene-transformed cells.
      Mol. Cell. Biol. (Life Sci. Adv.), 7: 1-7 (1988).
      


2099. Holý, A., Rosenberg, I., Dvorakova, H. & De Clercq, E.
      Synthesis and evaluation of acyclic nucleoside anlaogs.
      Nucleosides & Nucleotides, 7: 667-670 (1988).
      


2100. Marquardt, H., Westendorf, J., Schaefer, A., Boldt, J., De Clercq, E. & Marquardt, H.
      5-Substituted 2'-deoxyuridines: mutagenic and antimutagenic ef­fects.
      Arzneimittel-Forschung (Drug Research), 38: 1820-1824 (1988).
      


2101. Snoeck, R., Sakuma, T., De Clercq, E., Rosenberg, I. & Holý, A.
      (S)-1-(3-Hydroxy-2-phosphonylmethoxypropyl)cytosine [(S)-HPMPC]: a potent and selective inhibitor of human cy­tomegalovirus replication.
      Antimicrob. Agents Chemother., 32: 1839-1844 (1988).
      


2102. Baba, M., Schols, D., Pauwels, R., Balzarini, J. & De Clercq, E.
      Fuchsin acid selectively inhibits human immunodefi­ciency virus (HIV) replication in vitro.
      Biochem. Biophys. Res. Commun., 155: 1404-1411 (1988).
      


2103. Baba, M., Snoeck, R., Pauwels, R. & De Clercq, E.
      Sulfated polysaccharides are potent and selective inhibitors of various enveloped viruses, including herpes simplex virus, cy­tomegalovirus, vesicular stomatitis virus, and human immunodefi­ciency virus.
      Antimicrob. Agents Chemother., 32: 1742-1745 (1988).
      


2104. Burns, N.J. III, Barnett, B.B., Huffman, J.H., Daw­son, M.I., Sid­well, R.W., De Clercq, E. & Kende, M.
      A newly developed immunofluorescent assay for deter­mining the Pichinde virus-inhibi­tory effects of se­lected nucleoside ana­logues.
      Antiviral Res., 10: 89-98 (1988).
      


2105. Herdewijn, P., Balzarini, J., Baba, M., Pauwels, R., Van Aer­schot, A., Janssen, G. & De Clercq, E.
      Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides.
      J. Med. Chem., 31: 2040-2048 (1988).
      


2106. Puech, F., Gosselin, G., Balzarini, J., De Clercq, E. & Imbach, J.-L.
      Synthesis and biological evaluation of isomeric di­nucleoside monophosphates and monomethylphosphonates of 9-ß-D-arabinofura­nosyladenine and related analogues.
      J. Med. Chem., 31: 1897-1907 (1988).
      


2107. Griengl, H., Hayden, W., Penn, G., De Clercq, E. & Rosenwirth, B.
      Phosphonoformate and -acetate derivatives of 5-sub­stituted 2'-de­oxyuridines: synthesis and antiviral activity.
      J. Med. Chem., 31: 1831-1839 (1988).
      


2108. Maudgal, P.C. & De Clercq, E.
      Bromovinyldeoxyuridine (BVDU) treatment of herpetic eye infec­tions.
      Proceedings of the Seventh Congress of the European Society of Ophthalmology, Lisbon, Portugal, 16-20 May 1988.
      Excerpta Medica International Congress Series (No. 803), Oph­thalmology Today, L.N. Ferraz de Oliveira (ed.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 589-591 (1988).
      


2109. Ono, K., Nakane, H., Herdewijn, P., Balzarini, J. & De Clercq, E.
      Inhibitory effects of various derivatives of azidothymidine triphosphate on reverse transcriptase and DNA polymerases.
      Nucleic Acids Res., Symposium Series, no. 20: 5-6 (1988).
      


2110. Arzuza, O., García-Villalón, D., Tabarés, E., Gil-Fernández, C. & De Clercq, E.
      Inhibition of African swine fever virus DNA synthe­sis by (S)-9-(3-hydroxy-2-phos­phonylmethoxypropyl)adenine.
      Biochem. Biophys. Res. Commun., 154: 27-32 (1988).
      


2111. Torrence, P.F., Kinjo, J.-e., Lesiak, K., Balzarini, J. & De Clercq, E.
      AIDS dementia: synthesis and properties of a derivative of 3'-azido-3'-deoxythymidine (AZT) that may become "locked" in the central nervous system.
      FEBS Letters, 234: 135-140 (1988).
      


2112. Schols, D., Pauwels, R., Vanlangendonck, F., Balzarini, J. & De Clercq, E.
      A highly reliable and sensitive, flow cytometric/fluorometric as­say for evaluation of the anti-HIV activity of antiviral com­pounds in MT-4 cells.
      J. Immunol. Methods, 114: 27-32 (1988).
      


2113. De Clercq, E.
      Chemotherapeutic approach of AIDS.
      Verhandelingen, Koninklijke Academie voor Geneeskunde van Bel­gië, 50: 166-217 (1988).
      


2114. Nakane, H., Balzarini, J., De Clercq, E. & Ono, K.
      Differential inhibition of various deoxyribonucleic acid poly­merases by Evans Blue and aurintricarboxylic acid.
      Eur. J. Biochem., 177: 91-96 (1988).
      


2115. Baba, M., Nakajima, M., Schols, D., Pauwels, R., Balzarini, J. & De Clercq, E.
      Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro.
      Antiviral Res., 9: 335-343 (1988).
      


2116. Olofsson, S., Milla, M., Hirschberg, C., De Clercq, E. & Datema, R.
      Inhibition of terminal N- and O-glycosylation specific for her­pesvirus-infected cells. Mechanism of an inhibitor of sugar nu­cleotide transport across Golgi membranes.
      Virology, 166: 440-450 (1988).
      


2117. Pauwels, R., Balzarini, J., Schols, D., Baba, M., Desmyter, J., Rosenberg, I., Holý, A. & De Clercq, E.
      Phosphonylmethoxyethyl purine derivatives: a new class of anti-human immunodefi­ciency virus agents.
      Antimicrob. Agents Chemother., 32: 1025-1030 (1988).
      


2118. Pauwels, R., Balzarini, J., Baba, M., Snoeck, R., Schols, D., Herdewijn, P., Desmyter, J. & De Clercq, E.
      Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds.
      J. Virol. Methods, 20: 309-321 (1988).
      


2119. Shigeta, S., Konno, K., Yokota, T., Nakamura, K. & De Clercq, E.
      Comparative activities of several nucleoside analogs against in­fluenza A, B and C viruses in vitro.
      Antimicrob. Agents Chemother., 32: 906-911 (1988).
      


2120. Baba, M., Pauwels, R., Balzarini, J., Arnout, J., Desmyter, J. & De Clercq, E.
      Mechanism of inhibitory effect of dextran sulfate and heparin on the replication of human immunodeficiency virus in vitro.
      Proc. Natl. Acad. Sci. USA, 85: 6132-6136 (1988).
      


2121. Verhoeven, G., Cailleau, J. & De Clercq, E.
      Stimulatory effects of antiviral adenosine analogs on steroido­genesis in Leydig cells.
      J. Steroid Biochem., 31: 267-274 (1988).
      


2122. Balzarini, J., Baba, M., Pauwels, R., Herdewijn, P. & De Clercq, E.
      Anti-retrovirus activity of 3'-fluoro- and 3'-azido-substituted pyrimidine 2',3'-dideoxynu­cleoside analogues.
      Biochem. Pharmacol., 37: 2847-2856 (1988).
      


2123. Robins, M.J., Madej, D., Hansske, F., Wilson, J.S., Gosselin, G., Bergogne, M.-C., Imbach, J.-L., Balzarini, J. & De Clercq, E.
      Nucleic acid related compounds. 53. Synthesis and biological evaluation of 2'-deoxy-ß-D-threo-pentofuranosyl nucleosides. "Reversion to starting alcohol" in Barton-type reductions of thionocarbonates.
      Canad. J. Chem., 66: 1258-1262 (1988).
      


2124. Boryski, J., Golankiewicz, B. & De Clercq, E.
      Synthesis and antiviral activity of novel N-substituted deriva­tives of acyclovir.
      J. Med. Chem., 31: 1351-1355 (1988).
      


2125. De Clercq, E.
      Recent advances in the search for selective antiviral agents.
      In "Advances in Drug Research", vol. 17, B. Testa (ed.). Aca­demic Press Inc., London, pp. 1-59 (1988).
      


2126. De Clercq, E.
      Antiviral treatment for HIV infection.
      American Foundation for AIDS Research, AIDS/HIV Experimental Treatment Directory, 2: no. 1, 1-6 (1988) and no 2, 11-16 (1988).
      


2127. Balzarini, J., Herdewijn, P., Pauwels, R., Broder, S. & De Clercq, E.
      ,ß- and ß,-Methylene 5'-phosphate derivatives of 3'-azido-2',3'-dideoxythymidine-5'-triphosphate: correlation between affinity for reverse transcriptase, susceptibility to hy­droly­sis by phosphodiesterases, and anti-retrovirus activity.
      Biochem. Pharmacol., 37: 2395-2403 (1988).
      


2128. Chang, C., Schwepler, D., Decedue, C.J., Balzarini, J., De Clercq, E. & Mertes, M.P.
      Linear free energy relationship studies of enzyme active site binding: thymidylate syn­thase.
      J. Med. Chem., 31: 1141-1147 (1988).
      


2129. Keizer, H.J., Pauwels, R., Landuyt, W., Balzarini, J., Van der Schueren, E. & De Clercq, E.
      Combined effects of bromovinyldeoxyuridine and fractionated or continuous administration of 5-fluorouracil in P388 leukemia-bearing mice.
      Cancer Letters, 39: 217-223 (1988).
      


2130. Seela, F., Driller, H., Herdering, W. & De Clercq, E.
      Dodecanucleotides containing (E)-5-(2-bromovinyl)-2'-deo-xy-uri­dine: influence of a bulky major groove substituent on duplex stability and endodeoxyribonuclease EcoRI recognition.
      Nucleosides & Nucleotides, 7: 347-363 (1988).
      


2131. Durbin, R.K., De Clercq, E. & Stollar, V.
      SVLM21, a mutant of Sindbis virus able to grow in Aedes al­bopictus cells in the absence of methionine, shows increased sen­sitivity to S-adenosylhomocysteine hydrolase inhibitors such as Neplanocin A.
      Virology, 163: 218-221 (1988).
      


2132. De Clercq, E.
      Antiviral chemotherapy today and tomorrow.
      Proceedings of the "Ninth European Conference of Internal Medi-cine", Bologna, Italy, 6-9 May 1987.
      Ann. Méd. Interne, 139: 84-86 (1988).
      


2133. Balzarini, J., Baba, M., Pauwels, R., Herdewijn, P., Wood, S.G., Robins, M.J. & De Clercq, E.
      Potent and selective activity of 3'-azido-2,6-diaminopurine-2',3'-dideoxyriboside, 3'-fluoro-2,6-diaminopurine-2',3'-dideo-xyriboside, and 3'-fluoro-2',3'-dideoxyguanosine against human immunodeficiency virus.
      Mol. Pharmacol., 33: 243-249 (1988).
      


2134. De Clercq, E.
      Interactions of antiviral agents with viral DNA synthesis.
      Biochem. Pharmacol., 37: 1789-1790 (1988).
      


2135. Iigo, M., Araki, E., Nakajima, Y., Hoshi, A. & De Clercq, E.
      Enhancing effect of bromovinyldeoxyuridine on antitumor activity of 5-fluorouracil against adenocarcinoma 755 in mice. Increased therapeutic index and correlation with increased plasma 5-fluo­rouracil levels.
      Biochem. Pharmacol., 37: 1609-1613 (1988).
      


2136. Pauwels, R., Baba, M., Balzarini, J., Herdewijn, P., Desmyter, J., Robins, M.J., Zou, R., Madej, D. & De Clercq, E.
      Investigations on the anti-HIV activity of 2',3'-dideoxyadeno­sine ana­logues with modi­fications in either the pentose or purine moiety. Potent and selective anti-HIV activity of 2,6-diamino­purine 2',3'-dideoxyriboside.
      Biochem. Pharmacol., 37: 1317-1325 (1988).
      


2137. Balzarini, J. & De Clercq, E.
      Chemotherapie van AIDS.
      Tijdschr. Geneesk., 44: 313-328 (1988).
      


2138. Krowicki, K., Balzarini, J., De Clercq, E., Newman, R.A. & Lown, J.W.
      Novel DNA groove binding alkylators : design, synthesis and bio­logical evaluation.
      J. Med. Chem., 31: 341-345 (1988).
      


2139. De Clercq, E.
      Molecular targets for selective antiviral chemotherapy.
      In "Antiviral Drug Development. A Multidisciplinary Approach", E. De Clercq & R.T. Walker (eds.).
      NATO Advanced Study Institutes Series, Series A : Life Sciences, Plenum Press, New York and London, pp. 97-122 (1988).
      


2140. Shigeta, S. & De Clercq, E.
      Treatment (bromovinyldeoxyuridine) of varicella-zoster virus in­fections.
      In "Clinical Use of Antiviral Drugs", E. De Clercq (ed.).
      Series "Developments in Medical Virology", Y. Becker (ed.).
      Martinus Nijhoff Publishing/Kluwer Academic Publishers, Norwell, Mas­sachusetts, USA, pp. 145-157 (1988).
      


2141. Maudgal, P.C. & De Clercq, E.
      Treatment (bromovinyldeoxyuridine) of herpetic eye infections.
      In "Clinical Use of Antiviral Drugs", E. De Clercq (ed.).
      Series "Developments in Medical Virology", Y. Becker (ed.).
      Martinus Nijhoff Publishing/Kluwer Academic Publishers, Norwell, Mas­sachusetts, USA, pp. 39-48 (1988).
      


2142. Kimura, T., Nishizawa, T., Yoshimizu, M. & De Clercq, E.
      Inhibitory activity of (E)-5-(2-bromovinyl)-2'-deoxyuridine on the salmonid herpesvi­ruses, Oncorhynchus masou virus (OMV) and Herpes virus salmonis.
      Microbiol. Immunol., 32: 57-65 (1988).
      


2143. De Clercq, E.
      Nucleoside analogues in the chemotherapy of virus infections : recent developments.
      In "Applied Virology Research, Vol. 1. New Vaccines and Chemotherapy", E. Kurstak, R.G. Marusyk, F.A. Murphy & M.H.V. Van Regenmortel (eds.).
      Plenum Publishing Corporation, New York, pp. 219-232 (1988).
      


2144. Snoeck, R. & De Clercq, E.
      La chimiothérapie des infections à cytomégalovirus.
      Médecine et Maladies Infectieuses, Tome 1988: 79-84 (1988).
      


2145. Jones, A.S., Sayers, J.R., Walker, R.T. & De Clercq, E.
      Synthesis and antiviral properties of (E)-5-(2-bromovinyl)-2'-deoxycyti­dine-related compounds.
      J. Med. Chem., 31: 268-271 (1988).
      


2146. Balzarini, J., Baba, M., Pauwels, R., Herdewijn, P., De Clercq, E., Broder, S. & Johns, D.G.
      The in vitro and in vivo anti-retrovirus activity, and intra­cellular metabolism of 3'-azido-2',3'-dideoxythymidine and 2',3'-dideoxycytidine are highly dependent on the cell species.
      Biochem. Pharmacol., 37: 897-903 (1988).
      


2147. Hirota, K., Kitade, Y., Tomishi, T., Maki, Y. & De Clercq, E.
      Nucleosides. Part 6. New chemical modification of the ribosyl moiety in uridines; syn­thesis of 2,2'-anhydro-1-[5-deoxy-5-(substituted thio)-ß-D-arabinofuranosyl]uracil derivatives and their conversion into 3',5'-epithiopyrimidine nucleosides.
      J. Chem. Soc. Perkin Trans. I, 2233-2241 (1988).
      



84 publications in the year 1987



2148. Trousdale, M.D., Robin, J.B., Willey, D.E. & De Clercq, E.
      Intentional reactivation of latent ocular herpes infection du­ring BVDU therapy.
      Current Eye Research, 6: 1471-1477 (1987).
      


2149. De Clercq, E.
      Virus-drug resistance : thymidine kinase-deficient (TK-) mutants of her­pes simplex virus. Therapeutic approaches.
      Proceedings of the "Third International Symposium of Clinical Microbio­logy", Spoleto, Italy, 18-20 September 1986.
      Annali dell' Istituto Superiore di Sanita, 23: 841-848 (1987).
      


2150. De Clercq, E.
      Strategies in the development of antiviral agents.
      Proceedings of the Tenth International Congress of Pharmacology, Sydney, Australia, 23-28 August 1987.
      Excerpta Medical International Congress Series (No. 750), Phar­macology, M.J. Rand & C. Raper (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 631-642 (1987).
      


2151. Bubley, G.J., Balzarini, J., Crumpacker, C.S., De Clercq, E.
      & Schnipper, L.E.
      The effect of (E)-5-(2-bromovinyl)-2'-deoxyuirdine on DNA repair and mu­tagenesis of herpes simplex virus type I.
      Virology, 161: 242-244 (1987).
      


2152. De Clercq E., Sakuma, T., Baba, M., Pauwels, R., Balzarini, J., Maudgal, P.C., Votruba, I., Rosenberg, I. & Holý, A.
      Phosphonylmethoxyalkylpurines and -pyrimidines : a new class of broad-spectrum anti-DNA virus agents.
      In "Progress in Antimicrobial and Anticancer Chemotherapy" (Proceedings of the Fif­teenth International Congress of Chemotherapy, Istanbul, Turkey, 19-24 July 1987), Vol. 1, B. Berkarda & H.-P. Kuemmerle (eds.).
      ECOMED Verlagsgesellschaft mbH, Landsberg am Lech, Federal Re­public of Germany, pp. 33-35 (1987).
      


2153. De Clercq, E.
      Perspectives for the chemotherapy of AIDS.
      In Proceedings of the First International Workshop on "New Perspectives in Cancer Research", Halkis, Greece, 15-18 October 1987.
      Anticancer Res., 7: 1023-1038 (1987).
      


2154. Gil-Fernandez, C., Garcia-Villalon, D., De Clercq, E., Rosen­berg, I. & Holý, A.
      Phosphonylmethoxyalkylpurines and pyrimidines as inhibitors of African swine fever virus replication in vitro.
      Antiviral Res., 8: 273-282 (1987).
      


2155. De Clercq, E., Sakuma, T., Baba, M., Pauwels, R., Balzarini, J., Rosen­berg, I. & Holý, A.
      Antiviral activity of phosphonylmethoxyalkyl derivatives of purine and pyrimidines.
      Antiviral Res., 8: 261-272 (1987).
      


2156. De Fazio, G., Vicente, M. & De Clercq, E.
      Antiviral effects of dihydroxypropyladenine [(RS)-DHPA] and bro­movinyldeoxyuridine (BVDU) on plant viruses.
      Antiviral Res., 8: 163-169 (1987).
      


2157. Balzarini, J., Cooney, D.A., Dalal, M., Kang, G.-J., Cupp, J.E., De Clercq, E., Broder, S. & Johns, D.G.
      2',3'-Dideoxycytidine : regulation of its metabolism and anti-retroviral potency by natural pyrimidine nucleosides and by in­hibitors of pyrimi­dine nucleotide synthesis.
      Mol. Pharmacol., 32: 798-806 (1987).
      


2158. De Clercq, E. & Bernaerts, R.
      Specific phosphorylation of 5-ethyl-2'-deoxyuridine by herpes simplex virus-infected cells and incorporation into viral DNA.
      J. Biol. Chem., 262: 14905-14911 (1987).
      


2159. Votruba, I., Bernaerts, R., Sakuma, T., De Clercq, E., Merta, A., Rosen­berg, I. & Holý, A.
      Intracellular phosphorylation of broad-spectrum anti-DNA virus agent (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine and in­hibition of viral DNA synthesis.
      Mol. Pharmacol., 32: 524-529 (1987).
      


2160. Jelinek, E. & De Clercq, E.
      No embryotoxicity of (E)-5-(2-bromovinyl)-2'-deoxyuridine when compared to related nucleoside analogs in chick embryos.
      Folia Morphologica, 35: 374-380 (1987).
      


2161. Ashwell, M., Jones, A.S., Kumar, A., Sayers, J.R., Walker, R.T., Sakuma, T. & De Clercq, E.
      The synthesis and antiviral properties of (E)-5-(2-bromovinyl)-2'-de­oxyuridine-related compounds.
      Tetrahedron, 43: 4601-4608 (1987).
      


2162. Holý, A., König, J., Vesely, J., Cech, D., Votruba, I. & De Clercq, E.
      5'-O-Alkyl-5-fluorouridines : synthesis and biological activity.
      Coll. Czech. Chem. Commun., 52: 1589-1608 (1987).
      


2163. Balzarini, J. & De Clercq, E.
      Differential affinities of pyrimidine nucleoside analogues for de­oxythymidine and de­oxycytidine kinase determine their incorpo­ration into murine leukemia L1210 cells.
      Acta Biochim. Polon., 34: 63-77 (1987).
      


2164. Pauwels, R., Herdewijn, P., Balzarini, J., Baba, M., De Clercq, E., Van­deputte, P. & Desmyter, J.
      In search of antiviral compounds against the AIDS virus.
      In "Frontiers in Microbiology", E. De Clercq (ed.).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 308-313 (1987).
      


2165. Baba, M. & De Clercq, E.
      Selective inhibitory effects of (S)-9-(3-hydroxy-2-phosphonyl­methoxypropyl) adenine and 2'-nor-cGMP on the replication of ade­novirus in vitro.
      In "Frontiers in Microbiology", E. De Clercq (ed.).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 305-307 (1987).
      


2166. Sakuma, T., De Clercq, E., Bernaerts, R., Votruba, I. & Holý, A.
      Antiviral activity of (S)-9-(3-hydroxy-2-phosphonyl­methoxypro-pyl)adenine [(S)-HPMPA].
      In "Frontiers in Microbiology", E. De Clercq (ed.).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 300-304 (1987).
      


2167. Cools, M., Drach, J.C. & De Clercq, E.
      S-Adenosyl-L-homocysteine hydrolase as target enzyme for antivi­ral agents : studies with adenosine kinase-deficient rat cells.
      In "Frontiers in Microbiology", E. De Clercq (ed.).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 297-299 (1987).
      


2168. Desgranges, C., Razaka, G. & De Clercq, E.
      Therapeutic implications of the unusually long half-life of (E)-5-(2-bromovinyl)uracil (BVUra) in vivo.
      In "Frontiers in Microbiology", E. De Clercq (ed.).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 293-296 (1987).
      


2169. Bernaerts, R., Verbruggen, A. & De Clercq, E.
      Mechanisms of antiviral action of 5-substituted 2'-deoxyuridines: (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVDU) as compared to its carbocyclic analogue (C-IVDU).
      In "Frontiers in Microbiology", E. De Clercq (ed.).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 289-292 (1987).
      


2170. Herdewijn, P., Pauwels, R., De Clercq, E., Charubala, R. & Pflei­derer, W.
      2'-5'-Oligoadenylates (2-5A) as mediators of interferon action. Synthesis and biological activity of new 2-5A analogues.
      In "Frontiers in Microbiology", E. De Clercq (ed).
      Martinus Nijhoff Publishers, Dordrecht, The Netherlands, pp. 231-233 (1987).
      


2171. Herdewijn, P., Pauwels, R., Baba, M., Balzarini, J. & De Clercq, E.
      Synthesis and anti-HIV activity of various 2'- and 3'-substi­tuted 2',3'-dideoxyadenosines : a structure-activity analysis.
      J. Med. Chem., 30: 2131-2137 (1987).
      


2172. De Clercq, E.
      New selective antiviral agents active against the AIDS virus.
      Trends in Pharmacological Sciences (TIPS), 8: 339-345 (1987).
      


2173. Baba, M., Pauwels, R., Balzarini, J., Herdewijn, P., De Clercq, E. & Desmyter, J.
      Ribavirin antagonizes inhibitory effects of pyrimidine 2',3'-dideoxynu­cleosides but enhances inhibitory effects of purine 2',3'-dideoxynucleo­sides on replication of human immunodefi­ciency virus in vitro.
      Antimicrob. Agents Chemother., 31: 1613-1617 (1987).
      


2174. Honjo, M., Maruyama, T., Horikawa, M., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of phosphonopyrimidine and phospho­nopurine ribo­nucleosides.
      Chem. Pharm. Bull., 35: 3227-3234 (1987).
      


2175. Balzarini, J., De Clercq, E., Verbruggen, A., Ayusawa, D., Shimizu, K. & Seno, T.
      Thymidylate synthetase is the principal target enzyme for the cy­tostatic activity of (E)-5-(2-bromovinyl)-2'-deoxyuridine against murine mammary carcinoma (FM3A) cells trans­formed with the herpes simplex virus type 1 or type 2 thymidine kinase gene.
      Mol. Pharmacol., 32: 410-416 (1987).
      


2176. Bobek, M., Kavai, I. & De Clercq, E.
      Synthesis and biological activity of 5-(2,2-difluorovinyl)-2'-deoxyuri­dine.
      J. Med. Chem., 30: 1494-1497 (1987).
      


2177. De Clercq, E.
      Recent trends and development in antiviral chemotherapy.
      Proceedings of the "CHEMRAWN V Conference on Contributions of Chemistry to Health, The New Frontiers", Heidelberg, F.R.Germany, 22-26 September 1986, H. Machleidt (ed.).
      VCH Verlagsgesellschaft, Weinheim, Federal Republic of Germany.
      Vol. 2, pp. 121-143 (1987).
      


2178. Sagi, J., De Clercq, E., Szemzö, A., Csarnyi, A., Kovacs, T.& Ötvös, L.
      Incorporation of the carbocyclic analogue of (E)-5-(2-bro­movinyl)-2'-de­oxyuridine 5'-triphosphate into a synthetic DNA.
      Biochem. Biophys. Res. Commun., 147: 1105-1112 (1987).
      


2179. Bobek, M., An, S.-H., De Clercq, E. & Bernacki, R.J.
      2'-Fluorinated pyrimidine isonucleosides. Novel nucleoside analogs demonstrate thera­peutic activity in mice with tumors.
      Nucleic Acids Res., Symposium Series, no. 18: 5-7 (1987).
      


2180. Herdewijn, P., Charubala, R., Pauwels, R., De Clercq, E. & Pflei­derer, W.
      Synthesis and biological activity of 3'-modified 2'-5'adenylate trimers.
      Proceedings of the "Seventh International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Konstanz, Federal Repu­blic of Germany, 29 September-3 October 1986.
      Nucleosides & Nucleotides, 6: 443-444 (1987).
      


2181. Herdewijn, P., Charubala, R., Pauwels, R., De Clercq, E. & Pflei­derer, W.
      Synthesis and activity of oligonucleotides containing a biologi­cally ac­tive nucleoside at the 2' end.
      Proceedings of the "Seventh International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Konstanz, Federal Repu­blic of Germany, 29 September-3 October 1986.
      Nucleosides & Nucleotides, 6: 441-442 (1987).
      


2182. Cools, M., De Clercq, E. & Drach, J.C.
      Role of adenosine kinase in the biological (antiviral and anti­cellular) activities of adenosine analogues.
      Proceedings of the "Seventh International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Konstanz, Federal Repu­blic of Germany, 29 September-3 October 1986.
      Nucleosides & Nucleotides, 6: 423-424 (1987).
      


2183. Bernaerts, R. & De Clercq, E.
      Mechanism of antiviral activity of 5-ethyl-2'-deoxyuridine.
      Proceedings of the "Seventh International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Konstanz, Federal Repu­blic of Germany, 29 September-3 October 1986.
      Nucleosides & Nucleotides, 6: 421-422 (1987).
      


2184. De Clercq, E.
      Targets for the antiviral activity of pyrimidine and purine nu­cleoside analogues.
      Proceedings of the "Seventh International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Konstanz, Federal Repu­blic of Germany, 29 September-3 October 1986.
      Nucleosides & Nucleotides, 6: 197-207 (1987).
      


2185. Gosselin, G., Bergogne, M.-C., Imbach, J.-L., De Rudder, J. & De Clercq, E.
      Systematic synthesis and biological evaluation of - and ß-D-xylo- and lyxofuranonu­cleosides of the five naturally occurring nucleic acid bases.
      Proceedings of the "Seventh International Round Table on Nucleo­sides, Nucleotides and their Biological Applications", Konstanz, Federal Repu­blic of Germany, 29 September-3 October 1986.
      Nucleosides & Nucleotides, 6: 65-72 (1987).
      


2186. Lin, J.-C., De Clercq, E. & Pagano, J.S.
      Novel acyclic adenosine analogs inhibit Epstein-Barr virus repli­cation.
      Antimicrob. Agents Chemother., 31: 1431-1433 (1987).
      


2187. Baba, M., Pauwels, R., Balzarini, J., Herdewijn, P. & De Clercq, E.
      Selective inhibition of human immunodeficiency virus (HIV) by 3'-azido-2',3'-dideoxy­guanosine in vitro.
      Biochem. Biophys. Res. Commun., 145: 1080-1086 (1987).
      


2188. Kawana, F., Shigeta, S., Hosoya, M., Suzuki, H. & De Clercq, E.
      Inhibitory effects of antiviral compounds on respiratory syncy­tial virus replication in vitro.
      Antimicrob. Agents Chemother., 31: 1225-1230 (1987).
      


2189. De Clercq, E., Béres, J. & Bentrude, W.G.
      Potent activity of 5-fluoro-2'-deoxyuridine and related com­pounds against thymidine kinase-deficient (TK-) herpes simplex virus : targeted at thymidylate synthase.
      Mol. Pharmacol., 32: 286-292 (1987).
      


2190. Balzarini, J., Robins, M.J., Zou, R., Herdewijn, P. & De Clercq, E.
      The 2',3'-dideoxyriboside of 2,6-diaminopurine and its 2',3'-didehydro derivative inhibit the deamination of 2',3'-dideoxyadenosine, an in­hibitor of human immunodeficiency virus (HIV) replication.
      Biochem. Biophys. Res. Commun., 145: 277-283 (1987).
      


2191. Balzarini, J., Pauwels, R., Baba, M., Robins, M.J., Zou, R., Herdewijn, P. & De Clercq, E.
      The 2',3'-dideoxyriboside of 2,6-diaminopurine selectively in­hibits hu­man immunode­ficiency virus (HIV) replication in vitro.
      Biochem. Biophys. Res. Commun., 145: 269-276 (1987).
      


2192. Kit, S., Ichimura, H. & De Clercq, E.
      Differential metabolism of (E)-5-(2-iodovinyl)-2'-deoxyuridine (IVDU) by equine herpesvirus type 1- and herpes simplex virus-in­fected cells.
      Antiviral Res., 8: 41-51 (1987).
      


2193. Ito, M., Baba, M., Sato, A., Pauwels, R., De Clercq, E. & Shigeta, S.
      Inhibitory effect of dextran sulfate and heparin on the replica­tion of human immunode­ficiency virus (HIV) in vitro.
      Antiviral Res., 7: 361-367 (1987).
      


2194. Herdewijn, P., Balzarini, J., De Clercq, E., Pauwels, R., Baba, M., Broder, S. & Vander­haeghe, H.
      3'-Substituted 2',3'-dideoxynucleoside analogues as potential anti-HIV (HTLV-III/LAV) agents.
      J. Med. Chem., 30: 1270-1278 (1987).
      


2195. Balzarini, J., Kang, G.-J., Dalal, M., Herdewijn, P., De Clercq, E., Broder, S. & Johns, D.G.
      The anti-HTLV-III (anti-HIV) activity and cytotoxic activity of 2',3'-didehydro-2',3'-dideoxyribonucleosides : a comparison with their parental 2',3'-dideoxyribonucleosides.
      Mol. Pharmacol., 32: 162-167 (1987).
      


2196. Iigo, M., Yamaizumi, Z., Nishimura, S., Hoshi, A. & De Clercq, E.
      The antitumor potency of oral tegafur against adenocarcinoma 755 in mice is markedly enhanced by oral (E)-5-(2-bromovinyl)-2'-de­oxyuridine.
      Japan. J. Cancer Res. (Gann), 78: 409-413 (1987).
      


2197. Vinckier, F., Boogaerts, M., Declerck, D. & De Clercq, E.
      Chronic herpetic infection in an immunocompromised patient.
      Report of a case.
      J. Oral Maxillofacial Surg., 45: 723-728 (1987).
      


2198. Pauwels, R., De Clercq, E., Desmyter, J., Balzarini, J., Goubau, P., Herdewijn, P., Vanderhaeghe, H. & Vandeputte, M.
      Sensitive and rapid assay on MT-4 cells for detection of antivi­ral com­pounds against the AIDS virus.
      J. Virol. Methods, 16: 171-185 (1987).
      


2199. Rosenwirth, B., Streicher, W., De Clercq, E., Wanek, E., Schwarz, W. & Griengl, H.
      In vitro and in vivo antiviral activity of 2'-fluorinated arabino­sides of 5-(2-halo­alkyl)uracil.
      Antiviral Res., 7 : 271-287 (1987).
      


2200. Griengl, H., Wanek, E., Schwarz, W., Streicher, W., Rosenwirth, B. & De Clercq, E.
      2'-Fluorinated arabinosides of 5-(2-haloalkyl)uracil : synthesis and an­tiviral activity.
      J. Med. Chem., 30: 1199-1204 (1987).
      


2201. Yokota, T., Konno, K., Shigeta, S., Verbruggen, A. & De Clercq, E.
      Incorporation of (E)-5-(2-iodovinyl)-2'-deoxyuridine into deoxyribonu­cleic acids of varicella-zoster virus (TK+ and TK- strains)-infected cells.
      Mol. Pharmacol., 31: 493-499 (1987).
      


2202. Takaku, H., Ito, T., Yoshida, S., Aoki, T. & De Clercq, E.
      Synthesis and biological evaluation of some acyclic nucleoside cyclic phosphoramidate derivatives.
      Nucleosides & Nucleotides, 6: 793-802 (1987).
      


2203. Golankiewicz, B., Zeidler, J. & De Clercq, E.
      Synthesis and biological activity of C-acyclic nucleosides of imi­dazo[1,5-a]-1,3,5-tri­azines.
      Nucleosides & Nucleotides, 6: 663-678 (1987).
      


2204. Hilfenhaus, J., De Clercq, E., Köhler, R., Geursen, R. & Seiler, F.
      Combined antiviral effects of acyclovir or bromovinyldeoxyuri­dine and human immu­noglobulin in herpes simplex virus-infected mice.
      Antiviral Res., 7: 227-235 (1987).
      


2205. Osterhaus, A.D.M.E., Groen, J. & De Clercq, E.
      Selective inhibitory effects of (S)-9-(3-hydroxy-2-phosphonyl­methoxypropyl)adenine and 1-(2'-deoxy-2'-fluoro-ß-D-arabinofura­nosyl)-5-iodouracil on seal herpesvirus (phocid herpesvirus 1) infection in vitro.
      Antiviral Res., 7: 221-226 (1987).
      


2206. Ayisi, N.K., Wall, R.A., Wanklin, R.J., Machida, H., De Clercq, E. & Sacks, S.L.
      Comparative metabolism of E-5-(2-bromovinyl)-2'-deoxyuridine and 1-ß-D-arabinofu­ranosyl-E-5-(2-bromovinyl)uracil in herpes sim­plex virus-in­fected cells.
      Mol. Pharmacol., 31: 422-429 (1987).
      


2207. Iigo, M., Nakajima, Y., Hoshi, A. & De Clercq, E.
      Enhancing effect of bromovinyldeoxyuridine on antitumor activity of 5-fluorouracil and ftorafur against adenocarcinoma 755 in mice.
      Eur. J. Cancer Clin. Oncol., 23: 773-777 (1987).
      


2208. De Clercq, E.
      S-Adenosylhomocysteine hydrolase inhibitors as broad-spectrum an­tiviral agents.
      Biochem. Pharmacol., 36: 2567-2575 (1987).
      


2209. Gosselin, G., Bergogne, M.-C., De Rudder, J., De Clercq, E. & Im­bach, J.-L.
      Systematic synthesis and biological evaluation of - and ß-D-lyxofura­nosyl nucleosides of the five naturally occurring nu­cleic acid bases.
      J. Med. Chem., 30: 982-991 (1987).
      


2210. De Clercq, E.
      Antivirale chemotherapie.
      In "Medische Virologie" (vierde, herziene druk), red. J.B. Wil­terdink.
      Bohn, Scheltema & Holkema, Utrecht, pp. 290-311 (1987).
      


2211. Joniau, M., De Clercq, E. & De Cuyper, M.
      Binding of biscationic fluorochromes to pig brain tubulin.
      In "The Cytoskeleton in Cell Differentiation and Development" (Proceedings of the First International Symposium held in Granada, Spain, 21-25 April 1987), R.B. Maccioni & J. Aréchaga (eds.). ICSU Symposium Series vol. 8.
      IRL Press, Oxford, England, pp. 89-90 (1987).
      


2212. De Clercq, E.
      New antiviral agents.
      In "Trends in Medicinal Chemistry" (Proceedings of the Ninth In­ternational Symposium on Medicinal Chemistry, W.-Berlin, F.R.Germany, 14-18 September 1986). E. Mutschler & E. Winter­feldt (eds.).
      VCH Verlagsgesellschaft, Weinheim, Federal Republic of Germany, pp. 487-501 (1987).
      


2213. Baba, M., Konno, K., Shigeta, S. & De Clercq, E.
      In vitro activity of (S)-9-(3-hydroxy-2-phosphonyl­methoxypropyl)-adenine against newly isolated clinical varicella-zoster virus strains.
      Eur. J. Clin. Microbiol., 6: 158-160 (1987).
      


2214. Baba, M., Mori, S., Shigeta, S. & De Clercq, E.
      Selective inhibitory effect of (S)-9-(3-hydroxy-2-phosphonyl­methoxypropyl)adenine and 2'-nor-cyclic GMP on adenovirus repli­cation in vitro.
      Antimicrob. Agents Chemother., 31: 337-339 (1987).
      


2215. Baba, M., Shigeta, S. & De Clercq, E.
      Serum and urine concentrations of oral bromovinyldeoxyuridine in humans as monitored by a bioassay system based on varicella-zoster virus focus inhibition.
      J. Med. Virol., 22: 17-23 (1987).
      


2216. Gil-Fernandez, C. & De Clercq, E.
      Comparative efficacy of broad-spectrum antiviral agents as in­hibitors of African swine fever virus replication in vitro.
      Antiviral Res., 7: 151-160 (1987).
      


2217. De Clercq, E.
      Antiviral chemotherapy : potential drugs for the treatment of se­vere virus infections.
      In "Update in Intensive Care and Emergency Medicine 1987", J.L. Vincent (ed.).
      Springer-Verlag, Berlin, Heidelberg, pp. 77-85 (1987).
      


2218. Keppeler, K. & De Clercq, E.
      Synthese und antivirale Aktivität von 2,3(1H,4H)-Chinoxalindion-Derivaten.
      Arch. Pharm., 320: 271-274 (1987).
      


2219. Maudgal, P.C., De Clercq, E. & Huyghe, P.
      Experimental thymidine kinase-deficient HSV-1 keratitis : thera­peutic at­tempts.
      Current Eye Research, 6: 579-584 (1987).
      


2220. Jones, A.S., McClean, M.J., Slater, M.J., Walker, R.T., Balzarini, J. & De Clercq, E.
      Synthesis of 5-(1-substituted ethyl)uracil derivatives and some of their chemical and biological properties.
      J. Chem. Soc. Perkin Trans. I, 1987: 457-464 (1987).
      


2221. Ito, M., Nakashima, H., Baba, M., Pauwels, R., De Clercq, E., Shigeta, S. & Yamamoto, N.
      Inhibitory effect of glycyrrhizin on the in vitro infectivity and cy­topathic activity of the human immunodeficiency virus [HIV (HTLV-III/LAV)].
      Antiviral Res., 7: 127-137 (1987).
      


2222. Baba, M., Pauwels, R., Herdewijn, P., De Clercq, E., Desmyter, J. & Vandeputte, M.
      Both 2',3'-dideoxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidi­nene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro.
      Biochem. Biophys. Res. Commun., 142: 128-134 (1987).
      


2223. Gupta, S.V., Tourigny, G., Stuart, A.L., De Clercq, E., Quail, J.W., Ekiel, I., El-Kabbani, O.A.L. & Delbaere, L.T.J.
      Relationship between structure and antiviral activity of 5-methoxymethyl-2'-deoxyuridine and 5-methoxymethyl-1-(2'-deoxy-ß-D-lyxo­furanosyl)uracil.
      Antiviral Res., 7: 69-77 (1987).
      


2224. De Clercq, E.
      Antiviral nucleoside analogs.
      ISI Atlas of Science, Pharmacology, 1: 20-24 (1987).
      


2225. Kit, S., Ichimura, H. & De Clercq, E.
      Phosphorylation of nucleoside analogs by equine herpesvirus type 1 pyrimidine deoxy­ribonucleoside kinase.
      Antiviral Res., 7: 53-67 (1987).
      


2226. Al-Razzak, L.A., Schwepler, D., Decedue, C.J., Balzarini, J., De Clercq, E. & Mertes, M.P.
      5-Quinone derivatives of 2'-deoxyuridine 5'-phosphate : inhibi­tion and inactivation of thymidylate synthase, antitumor cell, and antiviral studies.
      J. Med. Chem., 30: 409-419 (1987).
      


2227. De Clercq, E., Balzarini, J., Madej, D., Hansske, F. & Robins, M.J.
      Nucleic acid related compounds. 51. Synthesis and biological properties of sugar-modi­fied analogues of the nucleoside anti­biotics tubercidin, toyocamycin, sangivamycin, and formycin.
      J. Med. Chem., 30: 481-486 (1987).
      


2228. Birnbaum, G.I., De Clercq, E., Hatfield, P.W. & Robins, M.J.
      Synthesis and conformational studies of 4-carbamoyl-1[(2-hydro­xyethoxy)methyl]-5-(methylamino)imidazole and derivatives as new acy­clonucleoside analogues.
      Heterocycles, 25: 493-506 (1987).
      


2229. Maudgal, P.C., De Clercq, E. & Huyghe, P.
      Efficacy of (S)-HPMPA against thymidine kinase-deficient herpes simplex virus-keratitis.
      Invest. Ophthalmol. Visual Science, 28: 243-248 (1987).
      


2230. De Clercq, E.
      Suramin in the treatment of AIDS : mechanism of action.
      Antiviral Res., 7: 1-10 (1987).
      


2231. De Clercq, E.
      Antiviral agents in the treatment of herpes virus infections in immuno­suppressed patients.
      In "Antibiosis and Host Immunity" (Proceedings of the Interna­tional Symposium on Antimicrobial Agents and Immunity, held in Siena, Italy, 2-4 May 1985). A. Szentivanyi, H. Friedman & G. Gillissen (eds.).
      Plenum Publishing Corporation, New York, USA, pp. 123-134 (1987).
      



46 publications in the year 1986



2232. Ben-Efraim, S., Shoval, S. & De Clercq, E.
      Enhancing effect of bromovinyldeoxyuridine on antitumour acti­vity of 5-fluorouracil in mice bearing MOPC-315 plasmacytomas.
      Brit. J. Cancer, 54: 847-852 (1986).
      


2233. Blough, H.A., Pauwels, R., De Clercq, E., Cogniaux, J., Sprecher-Gold­berger, S. & Thiry, L.
      Glycosylation inhibitors block the expression of LAV/HTLV-III (HIV) gly­coproteins.
      Biochem. Biophys. Res. Commun., 141: 33-38 (1986).
      


2234. Holý, A., Votruba, I., Merta, A., De Clercq, E., Jelinek, R., Slama, K., Benes, K. & Melichar, O.
      Biological consequences of S-adenosyl-L-homocysteinase inhibi­tion by acyclic adeno­sine analogs.
      In "Biological Methylation and Drug Design. Experimental and Clinical Role of S-Adenosylmethionine", R.T. Borchardt, C.R. Creveling & P.M. Ue­land (eds.).
      Humana Press Inc., Clifton, New Jersey, USA, pp. 397-408 (1986).
      


2235. Balzarini, J., De Clercq, E., Verbruggen, A., Crumpacker, C., Ayusawa, D. & Seno, T.
      Increased sensitivity of thymidine kinase-deficient (TK-) tumor cell lines to the cell growth inhibitory effects of (E)-5-(2-bro­movinyl)-2'-deoxyuridine (BVDU) and related compounds.
      Anticancer Res., 6: 1077-1084 (1986).
      


2236. De Clercq, E. & Robins, M.J.
      Xylotubercidin against herpes simplex virus type 2 in mice.
      Antimicrob. Agents Chemother., 30: 719-724 (1986).
      


2237. De Clercq, E. & Herdewijn, P.
      Selektieve antivirale verbindingen.
      Pharmaceutisch Weekblad, 121: 916-921 (1986).
      


2238. Nakane, H., Balzarini, J., De Clercq, E. & Ono, K.
      Differential inhibitory effects of Evans Blue on various DNA poly­merases.
      Nucleic Acids Res., Symposium Series, no. 17: 183-186 (1986).
      


2239. Simizu, K., Ren, L., Ayusawa, D., Seno, T., Balzarini, J. & De Clercq, E.
      Establishment of mutant murine mammary carcinoma FM3A cell strains transformed with the herpes simplex virus type 2 thymi­dine kinase gene.
      Cell Structure and Function, 11: 295-301 (1986).
      


2240. Maudgal, P.C., De Clercq, E., Bernaerts, R., Dieltiens, M., Breemersch, M. & Van Eeck­houtte, L.
      Ocular penetration and efficacy of chloroethyldeoxyuridine against her­petic kerato­uveitis.
      Invest. Ophthalmol. Visual Science, 27: 1453-1458 (1986).
      


2241. De Clercq, E.
      Chemotherapeutic approaches to the treatment of the acquired im­mune de­ficiency syn­drome (AIDS).
      J. Med. Chem., 29: 1561-1569 (1986).
      


2242. Schneller, S.W., May, J.L. & De Clercq, E.
      The synthesis and antiviral properties of 8-amino-3[(2-hydro­xyethoxy)-methyl]-1,2,4-triazo[4,3-a]pyrazine.
      Croatica Chemica Acta, 59: 307-311 (1986).
      


2243. De Clercq, E.
      Antiviral chemotherapy : acquired immune deficiency syndrome.
      Proceedings of the IXth International Congress of Infectious and Para­sitic Diseases, Munich, F.R.Germany, 20-26 July 1986, Volume 1. Viral Infections, W. Marget, W. Lang & E. Gabler-Sandberger (eds.).
      MMV Medizin Verlag, München, Federal Republic of Germany, pp. 211-215 (1986).
      


2244. Shigeta, S., Mori, S., Yokota, T., Konno, K. & De Clercq, E.
      Characterization of a varicella-zoster virus variant with al­tered thymi­dine kinase activity.
      Antimicrob. Agents Chemother., 29: 1053-1058 (1986).
      


2245. Baba, M., Konno, K., Shigeta, S. & De Clercq, E.
      Inhibitory effects of selected antiviral compounds on newly iso­lated clinical varicella-zoster virus strains.
      Tohoku J. Exp. Med., 148: 275-283 (1986).
      


2246. Belmans, M., Vrijens, Y., Esmans, E., Dommisse, R., Lepoivre, J., Alder­weireldt, F., Townsend, L.B., Wotring, L.L., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of a series of substituted 2-pyri­dine-C-nucleosides. Part II.
      Nucleosides & Nucleotides, 5: 441-455 (1986).
      


2247. De Clercq, E.
      Potential of bromovinyldeoxyuridine in anticancer chemotherapy.
      In "Proceedings of the First International Conference of Anti­cancer Re­search", Loutraki, Greece, 26-30 October 1985, J.G. Delinassios (ed.).
      Anticancer Res., 6: 549-556 (1986).
      


2248. De Clercq, E.
      Towards a selective chemotherapy of virus infections. Develop­ment of bromovinylde­oxyuridine as a highly potent and selective anti-herpetic drug.
      Verhandelingen, Koninklijke Academie voor Geneeskunde van Bel­gië, 48: 261-290 (1986).
      


2249. Lown, J.W., Krowicki, K., Balzarini, J. & De Clercq, E.
      Structure-activity relationship of novel oligopeptide antiviral and an­titumor agents related to netropsin and distamycin.
      J. Med. Chem., 29: 1210-1214 (1986).
      


2250. Balzarini, J., Pauwels, R., Herdewijn, P., De Clercq, E., Cooney, D.A., Kang, G.-J., Dalal, M., Johns, D.G. & Broder, S.
      Potent and selective anti-HTLV-III/LAV activity of 2',3'-dideoxycy­tidinene, the 2',3'-unsaturated derivative of 2',3'-dideoxycytidine.
      Biochem. Biophys. Res. Commun., 140: 735-742 (1986).
      


2251. Scheck, A.C., Wigdahl, B., De Clercq, E. & Rapp, F.
      Prolonged herpes simplex virus latency in vitro after treat­ment of in­fected cells with acyclovir and human leukocyte inter­feron.
      Antimicrob. Agents Chemother., 29: 589-593 (1986).
      


2252. Balzarini, J., Mitsuya, H., De Clercq, E. & Broder, S.
      Aurintricarboxylic acid and Evans Blue represent two different classes of anionic com­pounds which selectively inhibit the cy­topathogenicity of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus.
      Biochem. Biophys. Res. Commun., 136: 64-71 (1986).
      


2253. Defilippi, P., Huez, G., Verhaegen-Lewalle, M., De Clercq, E., Imai, J., Torrence, P.F. & Content, J.
      Antiviral activity of a chemically stabilized 2-5A analog upon microin­jection into HeLa cells.
      FEBS Letters, 198: 326-332 (1986).
      


2254. De Clercq, E.
      Current trends in antiviral chemotherapy.
      J. Antimicrob. Chemother., 17: 399-402 (1986).
      


2255. De Clercq, E., Holý, A., Rosenberg, I., Sakuma, T., Balzarini, J. & Maudgal, P.C.
      A novel selective broad-spectrum anti-DNA virus agent.
      Nature, 323: 464-467 (1986).
      


2256. Desgranges, C., De Clercq, E., Razaka, G., Drouillet, F., Bel­loc, I. & Bricaud, H.
      Deoxyribosyl exchange reactions leading to the in vivo genera­tion and regeneration of the antiviral agents (E)-5-(2-bro­movinyl)-2'-deoxyuridine, 5-ethyl-2'-deoxyuridine and 5-(2-chloroethyl)-2'-deoxyuridine.
      Biochem. Pharmacol., 35: 1647-1653 (1986).
      


2257. Ayisi, N.K., Wall, R.A., De Clercq, E. & Sacks, S.L.
      High performance liquid chromatographic analysis of (E)-5-(2-bro­movinyl)-2'-deoxyuridine and its metabolites in serum, urine and herpes simplex virus type-1 infected cells.
      J. Chromatogr., 375: 423-430 (1986).
      


2258. De Clercq, E. & Walker, R.T.
      Chemotherapeutic agents for herpesvirus infections.
      In "Progress in Medicinal Chemistry", Vol. 23, G.P. Ellis & G.B. West (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 187-218 (1986).
      


2259. Pauwels, R., De Clercq, E., Balzarini, J., Sawai, H., Imbach, J.L., Gos­selin, G., Huss, S., Reese, C.B., Serafinowska, H., Nor­man, D.G., Pflei­derer, W., Mikhailov, S.N. & Tor­rence, P.F.
      Biological activity of new 2-5A analogues.
      Proceedings of the Second International Congress on "Synthetic Oligonu­cleotides in Molecular Biology", Uppsala, Sweden, 18-24 August 1985.
      Chemica Scripta, 26: 141-145 (1986).
      


2260. De Clercq, E.
      Targeted development of new antiviral agents.
      Proceedings of the Second International Congress on "Synthetic Oligonu­cleotides in Molecular Biology", Uppsala, Sweden, 18-24 August 1985.
      Chemica Scripta, 26: 41-47 (1986).
      


2261. Keppeler, K., Kiefer, G. & De Clercq, E.
      Synthesis and antiviral activity of acyclic derivatives of 5-ethyl-2'-deoxyuridine.
      Arch. Pharm., 319: 360-365 (1986).
      


2262. De Clercq, E.
      Antiviral agents and the immune system.
      In "Antimicrobial Agents and Immunity", J. Jeljaszewicz & G. Pulverer (eds.). Academic Press Inc., London, pp. 19-65 (1986).
      


2263. Verbruggen, A., Julien, C., De Clercq, E. & De Roo, M.
      Simple quantitative radioiodination of (E)-5-(2-iodovinyl)-2'-deoxyuri­dine (IVDU) by exchange labelling.
      Int. J. Appl. Radiat. Isotop., 37: 355-357 (1986).
      


2264. Béres, J., Sagi, G., Bentrude, W.G., Balzarini, J., De Clercq, E. & Ötvös, L.
      Synthesis and antitumor and antiviral properties of 5-halo- and 5-(trifluoromethyl)-2'-deoxyuridine 3',5'-cyclic monophosphates and neu­tral triesters.
      J. Med. Chem., 29: 1243-1249 (1986).
      


2265. Béres, J., Bentrude, W.G., Balzarini, J., De Clercq, E. & Ötvös, L.
      Synthesis and antitumor and antiviral properties of 5-alkyl-2'-de­oxyuridines, 3',5'-cyclic monophosphates and neutral cyclic triesters.
      J. Med. Chem., 29: 494-499 (1986).
      


2266. Béres, J., Bentrude, W.G., Kalman, A., Parkanyi, L., Balzarini, J. & De Clercq, E.
      Synthesis, structure and antitumor and antiviral activities of a series of 5-halouridine cyclic 3',5'-monophosphates.
      J. Med. Chem., 29: 488-493 (1986).
      


2267. De Clercq, E., Bernaerts, R., Bergstrom, D.E., Robins, M.J., Montgomery, J.A. & Holý, A.
      Antirhinovirus activity of purine nucleoside analogues.
      Antimicrob. Agents Chemother., 29: 482-487 (1986).
      


2268. Desgranges, C., Razaka, G., De Clercq, E., Herdewijn, P., Balzarini, J., Drouillet, F. & Bricaud, H.
      Effect of (E)-5-(2-bromovinyl)uracil on the catabolism and anti­tumor ac­tivity of 5-fluorouracil in rats and leukemic mice.
      Cancer Res., 46: 1094-1101 (1986).
      


2269. Balzarini, J., Mitsuya, H., De Clercq, E. & Broder, S.
      Comparative inhibitory effects of suramin and other selected com­pounds on the infec­tivity and replication of human T-cell lym­photropic virus (HTLV-III)/lymphadenopathy-associated virus (LAV).
      Int. J. Cancer, 37: 451-457 (1986).
      


2270. Kitaoka, S., Konno, T. & De Clercq, E.
      Comparative efficacy of broad-spectrum antiviral agents as in­hibitors of rotavirus repli­cation in vitro.
      Antiviral Res., 6: 57-65 (1986).
      


2271. Kiefer, G., Keppeler, K. & De Clercq, E.
      Prodrugs of 5-ethyl-2'-deoxyuridine. II. Syntheses and antiviral activi­ties of 5'- and 3'-ester derivatives.
      Arch. Pharm., 319: 154-160 (1986).
      


2272. De Clercq, E., Desgranges, C., Herdewijn, P., Sim, I.S., Jones, A.S., McLean, M.J. & Walker, R.T.
      Synthesis and antiviral activity of (E)-5-(2-bromovinyl)uracil and (E)-5-(2-bromo­vinyl)uridine.
      J. Med. Chem., 29: 213-217 (1986).
      


2273. Gosselin, G., Bergogne, M.-C., De Rudder, J., De Clercq, E. & Im­bach, J.-L.
      Systematic synthesis and biological evaluation of - and ß-D-xylofura­nosyl nucleosides of the five naturally occurring bases in nucleic acids and related analogues.
      J. Med. Chem., 29: 203-213 (1986).
      


2274. De Clercq, E.
      Present trends in the development of antiviral agents.
      In "The Antimicrobial Agents Annual 1", P.K. Peterson & J. Ver­hoef (eds.).
      Elsevier Science Publishers, B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 526-537 (1986).
      


2275. De Clercq, E.
      Antivirale geneesmiddelen.
      In "Algemene Farmacotherapie" (vijfde druk), red. H. Wesseling & C. Neef.
      Samson Stafleu, Alphen aan den Rijn/Brussel, pp. 829-835 (1986).
      


2276. De Clercq, E. & Cassiman, J.J.
      Mutagenic potential of anti-herpes agents.
      Life Sci., 38: 281-289 (1986).
      


2277. Tricot, G., De Clercq, E., Boogaerts, M.A. & Verwilghen, R.
      Oral bromovinyldeoxyuridine therapy for herpes simplex and vari­cella-zoster virus in­fections in severely immunosuppressed pa­tients : a pre­liminary clinical trial.
      J. Med. Virol., 18: 11-20 (1986).
      



59 publications in the year 1985



2278. Yokota, T., Konno, K., Shigeta, S. & De Clercq, E.
      The inhibitory effect of halovinyl deoxyuridine on varicella-zoster virus replication and deoxynucleoside metabolism.
      In "Recent Advances in Chemotherapy. Antimicrobial Sections" (Proceedings of the 14th International Congress of Chemotherapy, Kyoto, Japan, 21-28 June, 1985), J. Ishigami (ed.).
      University of Tokyo Press, pp. 1969-1970 (1985).
      


2279. Defilippi, P., Huez, G., Verhaegen-Lewalle, M., De Clercq, E., Torrence, P. & Content, J.
      Antiviral activity towards VSV and mengo virus of a chemically stabi­lized 2-5A analog upon microinjection into HeLa cells.
      In "The 2-5A System : Molecular and Clinical Aspects of the In­terferon Regulated Pathway" (Proceedings of the Sixth Interna­tional Symposium of the Research Institute, Hospital for Sick Children, Toronto, Ontario, Canada, 3-5 June, 1985), B.R.G. Williams & R.H. Silverman (eds.).
      Alan R. Liss, Inc., New York, pp. 141-146 (1985).
      


2280. Desgranges, C., Razaka, G., Belloc, I., Drouillet, F., De Clercq, E. & Bricaud, H.
      Inhibition de la dégradation de la 5-fluorouracile chez le rat.
      (Inhibition of the degradation of 5-fluorouracil in the rat).
      J. Pharm. Clin. 4 (hors série I): 97-105 (1985).
      


2281. De Clercq, E.
      Orofacial herpes simplex virus infections : therapeutic ap­proaches.
      J. Head Neck Pathol., 4: 141-145 (1985).
      


2282. Balzarini, J., De Clercq, E., Verbruggen, A., Ayusawa, D. & Seno, T.
      Highly selective cytostatic activity of (E)-5-(2-bromovinyl)-2'-de­oxyuridine derivatives for murine mammary carcinoma cells transformed with the herpes simplex virus type 1 thymidine ki­nase gene.
      Mol. Pharmacol., 28: 581-587 (1985).
      


2283. Jones, A.S., McLean, M.J., Tanaka, H., Walker, R.T., Balzarini, J. & De Clercq, E.
      The chemistry of 2',3'-seconucleosides. II. Reactions and bio­logical properties of 2',3'-secopyrimidine ribonucleosides.
      Tetrahedron, 41: 5965-5972 (1985).
      


2284. Jones, A.S., Walker, R.T., Wyatt, P.G., Balzarini, J. & De Clercq, E.
      The chemistry of 2',3'-seconucleosides. Part 1. Synthesis and chemical and biological properties of derivatives of 2',3'-se­couridine.
      J. Chem. Res. (S), 1985: 336-337 (1985).
      


2285. De Clercq, E.
      Synthetic pyrimidine nucleoside analogues.
      In "Approaches to Antiviral Agents", M.R. Harnden (ed.).
      The Macmillan Press Ltd., London, pp. 57-99 (1985).
      


2286. Ayusawa, D., Shimizu, K., Seno, T., Balzarini, J. & De Clercq, E.
      Establishment of mutant FM3A murine mammary carcinoma cell lines trans­formed with the herpes simplex virus type 1 thymidine ki­nase gene.
      Japan. J. Cancer Res. (Gann), 76: 984-988 (1985).
      


2287. Walker, R.T., Slater, M.J., Jones, A.S., Balzarini, J. & De Clercq, E.
      The synthesis and biological properties of some 5-substituted 2'-de­oxyuridines.
      Nucleic Acids Res., Symposium Series, no. 16 : 291-294 (1985).
      


2288. Balzarini, J., De Clercq, E., Ayusawa, D., Shimizu, K. & Seno, T.
      Selective inhibition of the proliferation of herpes simplex virus type 1 thymidine kinase gene-transformed murine mammary FM3A car­cinoma cells by (E)-5-(2-bromovinyl)-2'-deoxyuridine and related compounds.
      Nucleic Acids Res., Symposium Series, no. 16: 283-286 (1985).
      


2289. Lin, J.-C., Smith, M.C., Choi, E.I., De Clercq, E., Verbruggen, A. & Pagano, J.S.
      Effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine on replication of Ep­stein-Barr virus in human lymphoblastoid cell lines.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 121-126 (1985).
      


2290. De Clercq, E. & Balzarini, J.
      In search of specific inhibitors of retrovirus replication.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 89-94 (1985).
      


2291. Kawana, F., Shigeta, S. & De Clercq, E.
      Inhibitory effects of several antiviral compounds on the repli­cation of respiratory syn­cytial virus in vitro.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 83-88 (1985).
      


2292. Bernaerts, R., De Clercq, E., Balzarini, J., Herdewijn, P. & Ver­bruggen, A.
      Incorporation of carbocyclic (E)-5-(2-iodovinyl)-2'-deoxyuridine (C-IVDU) into DNA of herpes simplex virus-infected cells.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 51-56 (1985).
      


2293. Ayisi, N., Wall, R., De Clercq, E. & Sacks, S.
      Differential metabolism of (E)-5-(2-bromovinyl)-2'-deoxyuridine in wild-type and drug-resistant herpes simplex virus-infected cells.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May, 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 45-49 (1985).
      


2294. Shigeta, S., Yokota, T. & De Clercq, E.
      Therapy of varicella-zoster virus infection - mechanisms of ac­tion of (E)-5-(2-bromovi­nyl)-2'-deoxyuridine.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May, 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 35-44 (1985).
      


2295. Rosenwirth, B., Griengl, H., Wanek, E. & De Clercq, E.
      5-(2-Chloroethyl)-2'-deoxyuridine : a potent and selective in­hibitor of herpesviruses in vitro and in vivo.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May, 1985, A. Billiau, E. De Clercq & H. Schellekens, (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 21-28 (1985).
      


2296. De Clercq, E.
      Recent trends and developments in antiviral chemotherapy.
      In "Proceedings of the First International TNO Conference on An­tiviral Research", Rot­terdam, The Netherlands, 30 April-3 May, 1985, A. Billiau, E. De Clercq & H. Schellekens (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 11-19 (1985).
      


2297. De Clercq, E.
      Problems and new aspects of antiviral treatment : herpesvirus in­fections in immunosup­pressed patients.
      Infektionen bei Tumorpatienten [Infections in Cancer Patients (An Inter­national Per­spective)], Proceedings of the Symposium on "Prophylaxis and Treatment of Infections in Tumor Patients", München, Federal Republic of Germany, 30 March 1985, U. Jehn (ed.).
      W. Zuckschwerdt Verlag, München, Bern, Wien, pp. 91-114 (1985).
      


2298. Balzarini, J., De Clercq, E., Ayusawa, D. & Seno, T.
      Murine mammary FM3A carcinoma cells transformed with the herpes simplex virus type 1 thymidine kinase gene are highly sensitive to the growth-inhibitory properties of (E)-5-(2-bromovinyl)-2'-deoxyuridine and re­lated compounds.
      FEBS Letters, 185: 95-100 (1985).
      


2299. Maudgal, P.C. & De Clercq, E.
      Evaluation of bromovinyldeoxyuridine-related compounds in the treatment of experimen­tal herpes simplex keratitis.
      Arch. Ophthalmol., 103: 1393-1397 (1985).
      


2300. Herdewijn, P., Balzarini, J., De Clercq, E. & Vanderhaeghe, H.
      Resolution of aristeromycin enantiomers.
      J. Med. Chem., 28: 1385-1386 (1985).
      


2301. De Clercq, E. & Rosenwirth, B.
      Selective in vitro and in vivo activities of 5-(2-haloalkyl)pyrimidine nucleoside analogs, particularly 5-(2-chloroethyl)-2'-deoxyuridine, against herpes simplex virus.
      Antimicrob. Agents Chemother., 28: 246-251 (1985).
      


2302. De Clercq, E.
      Antiviral and antimetabolic activities of neplanocins.
      Antimicrob. Agents Chemother., 28: 84-89 (1985).
      


2303. Marquardt, H., Westendorf, J., De Clercq, E. & Marquardt, H.
      Potent anti-viral 5-(2-bromovinyl)-uracil nucleosides are inac­tive at in­ducing gene mu­tations in Salmonella typhimurium and V79 Chinese hamster cells and unscheduled DNA synthesis in pri­mary rat hepatocytes.
      Carcinogenesis, 6: 1207-1209 (1985).
      


2304. De Clercq, E. & Cools, M.
      Antiviral potency of adenosine analogues : correlation with in­hibition of S-adenosylho­mocysteine hydrolase.
      Biochem. Biophys. Res. Commun., 129: 306-311 (1985).
      


2305. De Clercq, E., Bernaerts, R., Balzarini, J., Herdewijn, P. & Ver­bruggen, A.
      Metabolism of the carbocyclic analogue of (E)-5-(2-iodovinyl)-2'-de­oxyuridine in her­pes simplex virus-infected cells.
      Incorporation of C-IVDU into DNA.
      J. Biol. Chem., 260: 10621-10628 (1985).
      


2306. Freeman, D.J., Sacks, S.L., De Clercq, E. & Spruance, S.L.
      Preclinical assessment of topical treatments for herpes simplex virus infection: 5 % (E)-5-(2-bromovinyl)-2'-deoxyuridine cream.
      Antiviral Res., 5: 169-177 (1985).
      


2307. Zhang, Z.-X., Dong, W.-P., Chen, H.-S., Xu, Z.-G., Zhang, Z.-H., Liu, S.-M. & De Clercq, E.
      Effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine on the growth and viral capsid antigen expression of Epstein-Barr virus-associated tumor (B-95-8) cells transplanted to nude mice.
      Proc. Soc. Exp. Biol. Med., 178: 616-622 (1985).
      


2308. De Clercq, E.
      Antiviral agents.
      In "Scientific Basis of Antimicrobial Chemotherapy", Symposium of the Society for General Microbiology, University of Notting­ham, England, 16-19 September, 1985, D. Greenwood & F.O'Grady (eds.).
      Cambridge University Press, Cambridge, England, pp. 155-184 (1985).
      


2309. Colla, L., Herdewijn, P., De Clercq, E., Balzarini, J. & Vander­haeghe, H.
      Synthesis and biological activity of 3'-azido and 3'-amino sub­stituted nucleoside ana­logs.
      Eur. J. Med. Chem., 20: 295-301 (1985).
      


2310. Belmans, M., Esmans, E., Dommisse, R., Lepoivre, J., Alder­weireldt, F., Balzarini, J. & De Clercq, E.
      Synthesis and biological evaluation of a series of substituted 2-pyri­dine C-nucleosides. I. Coupling reaction of organo-metal­lic pyridine compounds with 2,4:3,5-di-O-benzyl­idene-aldehydo-D-ri­bose.
      Nucleosides & Nucleotides, 4: 523-538 (1985).
      


2311. Vincent, P., Beaucourt, J.-P., Pichat, L., Balzarini, J. & De Clercq, E.
      Synthèses et activités biologiques de nouvelles (E)-alcènyl-5 désoxy-2' uridines.
      Nucleosides & Nucleotides, 4: 447463 (1985).
      


2312. Vincent, P., Beaucourt, J.-P., Pichat, L., Balzarini, J. & De Clercq, E.
      Synthèses, activités biologiques et étude conformationnelle d'alcynyl-5 désoxy-2' uridines.
      Nucleosides & Nucleotides, 4: 429-445 (1985).
      


2313. Balzarini, J., De Clercq, E., Herdewijn, P. & Robins, M.J.
      Role of thymidine kinase and thymidylate synthetase in the cyto­static, antimetabolic and antitumor effects of the carbocyclic analogue of 5-ni­tro-2'-deoxyuridine. A comparison with 5-nitro-2'-deoxyuridine.
      Mol. Pharmacol., 27: 578-583 (1985).
      


2314. Maudgal, P.C., Dieltiens, M., De Clercq, E. & Missotten, L.
      Oral bromovinyldeoxyuridine treatment of herpes zoster oph­thalmicus.
      Proceedings of the International Symposium on "Herpetic Eye Di­seases", Katholieke Universiteit Leuven, Belgium, 17-19 May, 1984, P.C. Maudgal & L. Missotten (eds.).
      Documenta Ophthalmologica, Vol. 44, Dr. W. Junk Publishers, Dor­drecht, The Nether­lands, pp. 403-407 (1985).
      


2315. Verbruggen, A.M., De Clercq, E., Maudgal, P.C., Ameye, C., Bus­son, R., Bernaerts, R., De Roo, M. & Missotten, L.
      Permeability of the cornea to [125I]IVDU, an analogue of bro­movinyldeoxyuridine.
      Proceedings of the International Symposium on "Herpetic Eye Di­seases", Katholieke Universiteit Leuven, Belgium, 17-19 May, 1984, P.C. Maudgal & L. Missotten (eds.).
      Documenta Ophthalmologica, Vol. 44, Dr. W. Junk Publishers, Dor­drecht, The Nether­lands, pp. 257-260 (1985).
      


2316. Maudgal, P.C., Dieltiens, M., De Clercq, E. & Missotten, L.
      Topical bromovinyldeoxyuridine treatment of herpes simplex ke­ratitis.
      Proceedings of the International Symposium on "Herpetic Eye Di­seases", Katholieke Universiteit Leuven, Belgium, 17-19 May, 1984, P.C. Maudgal & L. Missotten (eds.).
      Documenta Ophthalmologica, Vol. 44, Dr. W. Junk Publishers, Dor­drecht, The Nether­lands, pp. 247-255 (1985).
      


2317. De Clercq, E.
      New antiviral drugs for the treatment of herpesvirus infections.
      Proceedings of the International Symposium on "Herpetic Eye Di­seases", Katholieke Universiteit Leuven, Belgium, 17-19 May, 1984, P.C. Maudgal & L. Missotten (eds.).
      Documenta Ophthalmologica, Vol. 44, Dr. W. Junk Publishers, Dor­drecht, The Nether­lands, pp. 169-176 (1985).
      


2318. De Clercq, E.
      Targets for the antiviral and antitumor activities of nucleo­side, nu­cleotide and oligonu­cleotide analogues.
      Proceedings of the 6th International Round Table on Nucleosides, Nu­cleotides and their Biological Applications (held in La Grande Motte, France, on 9-12 October 1984).
      Nucleosides & Nucleotides, 4: 3-11 (1985).
      


2319. De Clercq, E.
      Inhibitors of reverse transcriptase and retrovirus replication.
      Arzneimittel-Forschung (Drug Research), 35: 1007-1008 (1985).
      


2320. Herdewijn, P., De Clercq, E., Balzarini, J. & Vanderhaeghe, H.
      Synthesis and antiviral activity of the carbocyclic analogues of (E)-5-(2-halogenovinyl)-2'-deoxyuridines and (E)-5-(2-haloge­novinyl)-2'-deoxy­cytidines.
      J. Med. Chem., 28: 550-555 (1985).
      


2321. De Clercq, E. & Holý, A.
      Alkyl esters of 3-adenin-9-yl-2-hydroxypropanoic acid : a new class of broad-spectrum antiviral agents.
      J. Med. Chem., 28: 282-287 (1985).
      


2322. De Clercq, E.
      Antiviral agents and immunity.
      Clin. Immunol. Newsletter, 6: 103-107 (1985).
      


2323. Yokota, T., Konno, K., Shigeta, S. & De Clercq, E.
      Incorporation of (E)-5-(2-bromovinyl)-2'-deoxyuridine into deoxyribonu­cleic acid of varicella-zoster virus (TK+- and TK-- strains)-infected cells.
      Proceedings of the International Symposium on "Herpes Viruses and Virus Chemothe­rapy, Pharmacological and Clinical Ap­proaches", Oiso, Japan, 10-13 September 1984, R. Kono & A. Naka­jima (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 237-238 (1985).
      


2324. Maudgal, P.C., De Clercq, E. & Missotten, L.
      Treatment of ocular herpes by new antiviral agents : in particu­lar acy­clovir (ACV) and bromovinyldeoxyuridine (BVDU).
      Proceedings of the International Symposium on "Herpes Viruses and Virus Chemothe­rapy, Pharmacological and Clinical Ap­proaches", Oiso, Japan, 10-13 September 1984, R. Kono & A. Naka­jima (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Netherlands, pp. 95-98 (1985).
      


2325. Shigeta, S., Kawaguchi, H., Konno, K., Yokota, T. & De Clercq, E.
      Susceptibility of several clinical isolates of varicella-zoster virus towards antiherpes drugs.
      Proceedings of the International Symposium on "Herpes Viruses and Virus Chemo­the­rapy, Pharmacological and Clinical Ap­proaches", Oiso, Japan, 10-13 September 1984, R. Kono & A. Naka­jima (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Nether­lands, pp. 81-84 (1985).
      


2326. De Clercq, E., Benoit, Y., Laureys, G. & Delbeke, M.J.
      Clinical potentials of bromovinyldeoxyuridine (BVDU) : in par­ticular for oral treat­ment of varicella-zoster virus infections in children with cancer.
      Proceedings of the International Symposium on "Herpes Viruses and Virus Chemo­therapy, Pharmacological and Clinical Ap­proaches", Oiso, Japan, 10-13 September 1984, R. Kono & A. Naka­jima (eds.).
      Elsevier Science Publishers B.V. (Biomedical Division), Amster­dam, The Nether­lands, pp. 49-52 (1985).
      


2327. De Clercq, E., Desgranges, C., Herdewijn, P., Sim, I.S. & Walker, R.T.
      Bromovinyluracil nucleoside analogues as antiherpes agents.
      Proceedings of the "VIIIth International Symposium on Medicinal Che­mistry", Uppsala, Sweden, 27-31 August 1984, Vol. 1, R. Dahlbom & J.L.G. Nilsson (eds.), Swedish Pharmaceutical Press, Stockholm, pp. 198-210 (1985).
      


2328. De Clercq, E.
      Antiherpesvirus agents and the immune system.
      Proceedings of the International Symposium on Antimicrobial Agents and Immunity, Heppenheim (W.-Germany), May 23-27, 1984.
      Zentralblatt für Bakt., Suppl. 13: 39-57 (1985).
      


2329. Holý, A., Votruba, I. & De Clercq, E.
      Structure-activity studies on open-chain analogues of nucleo­sides : inhibition of S-adenosyl-L-homocysteine hydrolase and antiviral activity. 2. Acid open-chain ana­logues.
      Collect. Czech. Chem. Commun., 50: 262-279 (1985).
      


2330. Holý, A., Votruba, I. & De Clercq, E.
      Structure-activity studies on open-chain analogues of nucleo­sides : inhibition of S-adenosyl-L-homocysteine hydrolase and antiviral activity. 1. Neutral open-chain ana­logues.
      Collect. Czech. Chem. Commun., 50: 245-261 (1985).
      


2331. Desgranges, C., Razaka, G., Bricaud, H. & De Clercq, E.
      Inhibition and reversal of the degradation of the antiviral drug (E)-5-(2-bromovinyl)-2'-deoxyuridine in vivo.
      Biochem. Pharmacol., 34: 405-406 (1985).
      


2332. Desgranges, C., Razaka, G., Bricaud, H. & De Clercq, E.
      Inhibition of the degradation of thymine and 5-substituted uracil analogues by (E)-5-(2-bromovinyl)uracil in vivo.
      Biochem. Pharmacol., 34: 403-404 (1985).
      


2333. Balzarini, J., De Clercq, E., Ayusawa, D. & Seno, T.
      Incorporation of 5-substituted pyrimidine nucleoside analogues into DNA of a thymidylate synthetase-deficient murine FM3A car­cinoma cell line.
      Methods and Findings in Experimental and Clinical Pharmacology, 7: 19-28 (1985).
      


2334. Maudgal, P.C., Verbruggen, A.M., De Clercq, E., Busson, R., Bernaerts, R., De Roo, M., Ameye, C. & Missotten, L.
      Ocular penetration of [125I]IVDU, a radiolabeled analogue of bromovinyl­deoxyuridine.
      Invest. Ophthalmol. Visual Science, 26: 45-49 (1985).
      


2335. Benoit, Y., Laureys, G., Delbeke, M.-J. & De Clercq, E.
      Oral BVDU treatment of varicella and zoster in children with cancer.
      Eur. J. Pediatr., 143: 198-202 (1985).
      


2336. De Clercq, E., Balzarini, J., Bernaerts, R., Herdewijn, P. & Verbruggen, A.
      Selective antiherpetic activity of carbocyclic analogues of (E)-5-(2-halogenovinyl)-2'-deoxyuridines : dependence on spe­cific phosphorylation by viral thymidine kinase.
      Biochem. Biophys. Res. Commun., 126: 397-403 (1985).
      



48 publications in the year 1984



2337. De Clercq, E., Content, J., Defilippi, P., Balzarini, J., War­rinnier, J., Sawai, H., Imai, J., Lesiak, K., Jamoulle, J.-C. & Torrence, P.F.
      Modes of action of interferon and analogues of 2-5A, a mediator of interferon action.
      In "IUPHAR 9th International Congress of Pharmacology London 1984" (Proceedings of the IXth International Congress of Phar­macology, held in London on 29 July-3 August, 1984), Sir William Patton, J. Mitchell & P. Turner (eds.).
      The Macmillan Press Ltd., London, pp. 307-317 (1984).
      


2338. De Clercq, E.
      Therapeutic potentials of bromovinyldeoxyuridine (BVDU) in the treatment of herpesvirus infections. II. Clinical aspects.
      In "Herpesvirus" UCLA Symposia on Molecular and Cellular Bio­logy, New Series, Vol. 21, F. Rapp (ed.).
      Alan R. Liss, Inc., New York, pp. 587-599 (1984).
      


2339. De Clercq, E.
      Therapeutic potentials of bromovinyldeoxyuridine (BVDU) in the treatment of herpesvirus infections. I. Fundamental aspects.
      In "Herpesvirus" UCLA Symposia on Molecular and Cellular Bio­logy, New Series, Vol. 21, F. Rapp (ed.).
      Alan R. Liss, Inc., New York, pp. 573-585 (1984).
      


2340. Wigdahl, B., Scheck, A.C., Smith, C.A., De Clercq, E. & Rapp, F.
      Herpes simplex virus latency and reactivation : design and analysis of in vitro con­structs.
      In "Herpesvirus" UCLA Symposia on Molecular and Cellular Bio­logy, New Series, Vol. 21, F. Rapp (ed.).
      Alan R. Liss, Inc., New York, pp. 121-144 (1984).
      


2341. Schneller, S.W., Luo, J.-K., Hosmane, R.S., De Clercq, E., Stoeckler, J.D., Agarwal, K.C., Parks, R.E.Jr. & Saunders, P.P.
      Synthesis and biological evaluation of 6-amino-IH-pyrrolo[3,2-c]pyridin-4(5H)-one (3,7-dideazaguanine).
      J. Med. Chem., 27: 1737-1739 (1984).
      


2342. De Clercq, E. & Walker, R.T.
      Synthesis and antiviral properties of 5-vinylpyrimidine nucleo­side analogs.
      Pharmacology and Therapeutics, 26: 1-44 (1984).
      


2343. Kulikowski, T., Zawadzki, Z., De Clercq, E. & Shugar, D.
      5-Substituted arabinofuranosyluracil nucleosides : synthesis and antiviral properties.
      Acta Biochim. Polon., 31: 341-356 (1984).
      


2344. Ayisi, N.K., De Clercq, E., Well, R.A., Hughes, H. & Sacks, S.L.
      Metabolic fate of (E)-5-(2-bromovinyl)-2'-deoxyuridine in her­pes simplex virus- and mock-infected cells.
      Antimicrob. Agents Chemother., 26: 762-765 (1984).
      


2345. Robins, M.J., Hatfield, P.W., Balzarini, J. & De Clercq, E.
      Nucleic acid related compounds. 47. Synthesis and biological activities of pyrimidine and purine "acyclic" nucleoside ana­logues.
      J. Med. Chem., 27: 1486-1492 (1984).
      


2346. Walker, R.T., Hunston, R.N., McGuigan, C., Jones, A.S., Balzarini, J. & De Clercq, E.
      Attempts to introduce biologically-active organic phosphates into living cells.
      In "Plenary Lectures of the Symposium on the Chemistry of He­terocyclic Compounds (VIIIth) and of Nucleic Acid Components (VIth) (held in Prague, Czechoslovakia, 2-8 September 1984), J. Beranek & E. Piskala (eds.).
      Institute of Macromolecular Chemistry, Czechoslovak Academy of Sciences, Prague, Czechoslovakia, pp. 23-34 (1984).
      


2347. De Clercq, E.
      Moderne Anti-HerpesMittel.
      Schwerpunkt Medizin, 7: 28-37 (1984).
      


2348. Yokota, T., Konno, K., Shigeta, S. & De Clercq, E.
      Comparative inhibition of DNA polymerases from varicella-zoster virus (TK+ and TK-) strains by (E)-5-(2-bromovinyl)-2'-de­oxyuridine 5'-triphosphate.
      Mol. Pharmacol., 26: 376-380 (1984).
      


2349. Torrence, P.F. & De Clercq, E.
      Preparation and biological properties of a highly active poly(G).poly(C) inducer of interferon.
      Antiviral Res., 4: 339-350 (1984).
      


2350. Maudgal, P.C., De Clercq, E. & Missotten, L.
      Efficacy of bromovinyldeoxyguanidine in the treatment of herpes simplex virus and varicella-zoster virus eye infections.
      Antiviral Res., 4: 281-291 (1984).
      


2351. Baba, M., Shigeta, S. & De Clercq, E.
      Influence of various experimental conditions on the inhibitory effects of E-5-(2-bro­movinyl)-2'-deoxyuridine on varicella-zoster virus replication in cell culture.
      Tohoku J. Exp. Med., 143: 441-449 (1984).
      


2352. Keppeler, K., Kiefer, G. & De Clercq, E.
      Prodrugs of 5-ethyl-2'-deoxyuridine. I. Syntheses and antiviral activity of some 5'-O-(acyl)-derivatives.
      Arch. Pharm., 317: 867-873 (1984).
      


2353. Balzarini, J., De Clercq, E., Ayusawa, D. & Seno, T.
      Thymidylate synthetase-positive and -negative murine mammary FM3A carcinoma cells as a useful system for detecting thymidy­late synthetase inhibitors.
      FEBS Letters, 173: 227-232 (1984).
      


2354. De Clercq, E.
      Antiherpes drugs : promises and pitfalls.
      Eur. J. Clin. Microbiol., 3: 96-107 (1984).
      


2355. De Clercq, E.
      Topical treatment of cutaneous herpes simplex virus infection in hairless mice with (E)-5-(2-bromovinyl)-2'-deoxyuridine and related compounds.
      Antimicrob. Agents Chemother., 26: 155-159 (1984).
      


2356. Siegel, S.A., Otto, M.J., De Clercq, E. & Prusoff, W.H.
      The effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine on synthesis of herpes simplex virus type 1-specific polypeptides.
      Antimicrob. Agents Chemother., 25: 566-570 (1984).
      


2357. Baba, M., Ito, M., Shigeta, S. & De Clercq, E.
      Synergistic antiviral effects of antiherpes compounds and human leukocyte interferon on varicella-zoster virus in vitro.
      Antimicrob. Agents Chemother., 25: 515-517 (1984).
      


2358. Hantz, O., Allaudeen, H.S., Ooka, T., De Clercq, E. & Trepo, C.
      Inhibition of human and woodchuck hepatitis virus DNA poly­merase by the triphos­phates of acyclovir, 1-(2'-deoxy-2'-fluoro-ß-D-arabinofuranosyl)-5-iodocytosine and E-5-(2-bro­movinyl)-2'-deoxyuridine.
      Antiviral Res., 4: 187-199 (1984).
      


2359. De Clercq, E., Bergstrom, D.E., Holý, A. & Montgomery, J.A.
      Broad-spectrum antiviral activity of adenosine analogues.
      Antiviral Res., 4: 119-133 (1984).
      


2360. Desgranges, C., Razaka, G., Drouillet, F., Bricaud, H., Herdewijn, P. & De Clercq, E.
      Regeneration of an antiviral drug (E)-5-(2-bromovinyl)-2'-de­oxyuridine (BVDU) in vivo.
      Nucleic Acids Res., 12: 2081-2090 (1984).
      


2361. Schneller, S.W., Thompson, R.D., Cory, J.G., Olsson, R.A., De Clercq, E., Kim, I.-K. & Chiang, P.K.
      Biological activity and a modified synthesis of 8-amino-3-(ß-D-ribofuranosyl)-1,2,4-triazolo[4,3-a]pyrazine, an isomer of formycin.
      J. Med. Chem., 27: 924-928 (1984).
      


2362. Jones, A.S., McGuigan, C., Walker, R.T., Balzarini, J. & De Clercq, E.
      Synthesis, properties and biological activity of some nucleo­side cyclic phosphorami­dates.
      J. Chem. Soc. Perkin Trans. I, 1471-1474 (1984).
      


2363. De Clercq, E.
      The antiviral spectrum of (E)-5-(2-bromovinyl)-2'-deoxyuridine.
      J. Antimicrob. Chemother., 14 (Suppl. A) : 85-95 (1984).
      


2364. De Clercq, E.
      Biochemical aspects of the selective antiherpes activity of nu­cleoside analogues.
      Biochem. Pharmacol., 33: 2159-2169 (1984).
      


2365. Percy, D.H., Creighton, M.O., Hatch, L.A. & De Clercq, E.
      Experimental herpetic keratitis in rabbit corneal organ cul­tures.
      Brit. J. Exp. Pathol., 65: 41-49 (1984).
      


2366. Wildiers, J. & De Clercq, E.
      Oral (E)-5-(2-bromovinyl)-2'-deoxyuridine treatment of severe herpes zoster in cancer patients.
      Eur. J. Cancer Clin. Oncol., 4: 471-476 (1984).
      


2367. Balzarini, J., De Clercq, E., Kiefer, G., Keppeler, K. & Buchele, A.
      Antitumor cell and antimetabolic effects of 5-ethyl-2'-de­oxyuridine and 5'-substituted 5-ethyl-2'-deoxyuridine deriva­tives.
      Investigational New Drugs, 2: 35-47 (1984).
      


2368. Zou, F.C., Dutschman, G.E., De Clercq, E. & Cheng, Y.-C.
      Differential binding affinities of sugar-modified derivatives of (E)-5-(2-bromovinyl)-2'-deoxyuridine for herpes simplex virus-induced and human cellular deoxythymidine kinases.
      Biochem. Pharmacol., 33: 1797-1800 (1984).
      


2369. Hunston, R.M., Jones, A.S., McGuigan, C., Walker, R.T., Balzarini, J. & De Clercq, E.
      Synthesis and biological properties of some cyclic phosphotri­esters derived from 2'-deoxy-5-fluorouridine.
      J. Med. Chem., 27: 440-444 (1984).
      


2370. Bergstrom, D.E., Brattesani, A.J., Ogawa, M.K., Reddy, P.A., Schweickert, M.J., Balzarini, J. & De Clercq, E.
      Antiviral activity of C-5 substituted tubercidin analogues.
      J. Med. Chem., 27: 285-292 (1984).
      


2371. Bergstrom, D.E., Ruth, J.L., Reddy, P.A. & De Clercq, E.
      Synthesis of (E)-5-(3,3,3-trifluoro-1-propenyl)-2'-deoxyuridine and related analogues : potent and unusually selective antivi­ral activity of (E)-5-(3,3,3-trifluoro-1-propenyl)-2'-deoxyuri­dine against herpes simplex virus type 1.
      J. Med. Chem., 27: 279-284 (1984).
      


2372. De Clercq, E.
      Bromovinyldeoxyuridine (BVDU) : current status in antiviral therapy.
      In "Control of Viral Diseases", (Proceedings of the IVth In­ternational Conference on Comparative Virology, Banff, Alberta, Canada, 17-22 October, 1982), E. Kurstak (ed.).
      Marcel Dekker Inc., New York and Basel, pp. 443-458 (1984).
      


2373. Balzarini, J., De Clercq, E., Ayusawa, D. & Seno, T.
      Thymidylate synthetase-deficient mouse FM3A mammary carcinoma cell line as a tool for studying the thymidine salvage pathway and the incorporation of thymidine ana­logues into host cell DNA.
      Biochem. J., 217: 245-252 (1984).
      


2374. Wigdahl, B., Scheck, A.C., Ziegler, R.J., De Clercq, E. & Rapp, F.
      Analysis of the herpes simplex virus genome during in vitro latency in human diploid fibroblasts and rat sensory neurons.
      J. Virol., 49: 205-213 (1984).
      


2375. Zhang, Z.-X., Liu, Y.-X., Chen, H.-S., Allaudeen, H.S. & De Clercq, E.
      Effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine on several pa­rameters of Epstein-Barr virus infection.
      J. Gen. Virol., 65: 37-46 (1984).
      


2376. Torrence, P.F. & De Clercq, E.
      Polynucleotide inducers of interferon : studies with poly(G). poly(C).
      In "Antiviral Drugs and Interferon : The Molecular Basis of their Activity", Y. Becker (ed.).
      Martinus Nijhoff Publishers, Boston and The Hague, pp. 317-333 (1984).
      


2377. De Clercq, E.
      BVDU [(E)-5-(2-bromovinyl)-2'-deoxyuridine].
      In "Antiviral Drugs and Interferon : The Molecular Basis of their Activity", Y. Becker (ed.).
      Martinus Nijhoff Publishers, Boston and The Hague, pp. 89-104 (1984).
      


2378. Balzarini, J. & De Clercq, E.
      Strategies for the measurement of the inhibitory effects of thymidine analogs on the activity of thymidylate synthase in intact murine leukemia L1210 cells.
      Biochim. Biophys. Acta, 785: 36-45 (1984).
      


2379. Pavan-Langston, D., Park, N.-H. & De Clercq, E.
      In vitro effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine, 5'-amino-5-iodo-2',5'-dide­oxyuridine and 2-deoxy-D-glucose on la­tent ganglionic herpes simplex virus infec­tion.
      Antiviral Res., 4: 53-61 (1984).
      


2380. De Clercq, E. & Torrence, P.F.
      Poly(G).poly(C) as an inducer of interferon.
      In "Physiology and Pathology of Interferon System", L. Borecky & V. Lackovic (eds).
      Volume 20 "Contributions to Oncology", S. Eckhardt, J.H. Holzner & G.A. Nagel (eds). S. Karger AG, Basel, pp. 375-386 (1984).
      


2381. Torrence, P.F., Imai, J., Lesiak, K., Jamoulle, J.-C., Sawai, H., Warrinnier, J., Balza­rini, J. & De Clercq, E.
      Strategies in the design of oligonucleotides as potential an­tiviral agents.
      In "Targets for the Design of Antiviral Agents", E. De Clercq & R.T. Walker (eds.). NATO Advanced Study Institutes Series, Series A : Life Sciences. Vol. 73, Plenum Press, New York and London, pp. 259-285 (1984).
      


2382. De Clercq, E.
      Pyrimidine nucleoside analogues as antiviral agents.
      In "Targets for the Design of Antiviral Agents", E. De Clercq & R.T. Walker (eds.). NATO Advanced Study Institutes Series, Series A : Life Sciences. Vol. 73, Plenum Press, New York and London, pp. 203-230 (1984).
      


2383. Maudgal, P.C., De Clercq, E., Descamps, J. & Missotten, L.
      Topical treatment of experimental herpes simplex keratouveitis with 2'-O-glycylacy­clovir. A water-soluble ester of acyclovir.
      Arch. Ophthalmol., 102: 140-142 (1984).
      


2384. Torrence, P.F. & De Clercq, E.
      Interferon induction by nucleic acids : structure-activity re­lationships.
      In "Handbook of Experimental Pharmacology", G.V.R. Born, A.E. Farah, H. Herken & A.D. Welch (eds.).
      Volume 71, "Interferons and their Applications", P.E. Came & W.A. Carter (eds.), Springer-Verlag, Berlin, Heidelberg and New York, pp. 233-258 (1984).
      



32 publications in the year 1983



2385. Kaufman, H.E., Varnell, E.D., Centifanto-Fitzgerald, Y.M., De Clercq, E. & Kissling, G.E.
      Oral antiviral drugs in experimental herpes simplex keratitis.
      Antimicrob. Agents Chemother., 24: 888-891 (1983).
      


2386. De Clercq, E., Hermann, D. & Guschlbauer, W.
      Interferon induction by platinum (II)-poly(I).poly(C) com­plexes.
      Biochim. Biophys. Acta, 741: 358-363 (1983).
      


2387. Desgranges, C., Razaka, G., Rabaud, M., Bricaud, H., Balzarini, J. & De Clercq, E.
      Phosphorolysis of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and other 5-substi­tuted 2'-deoxyuridines by purified human thymidine phosphorylase and intact blood platelets.
      Biochem. Pharmacol., 32: 3583-3590 (1983).
      


2388. Torrence, P.F., Imai, J., Lesiak, K., Warrinnier, J., Balzarini, J. & De Clercq, E.
      Structure-activity relationships for a potentiation of the an­timitogenic activity of 2-5A core derived from 2-5A, a mediator of interferon action.
      J. Med. Chem., 26: 1674-1678 (1983).
      


2389. Wittek, A.E., Cohen, P.S., Arvin, A.M., Smith, S.D., Koropchak, C.M. & De Clercq, E.
      Effects of (E)-5-(2-bromovinyl)-2'-deoxyuridine on prolifera­tion of human fibro­blasts, peripheral blood mononuclear cells, and granulocyte monocyte progenitor cells in vitro.
      Antimicrob. Agents Chemother., 24: 803-806 (1983).
      


2390. Boisjoly, H.M., Park, N.-H., Pavan-Langston, D. & De Clercq, E.
      Herpes simplex acyclovir resistant mutant in experimental kera­touveitis.
      Arch. Ophthalmol., 101: 1782-1786 (1983).
      


2391. Ono, K., Nakane, H., Colla, L. & De Clercq, E.
      Inhibition of terminal deoxynucleotidyltransferase by (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate.
      Nucleic Acids Res., Symposium Series, no. 12: 123-126 (1983).
      


2392. Balzarini, J. & De Clercq, E.
      Inhibitory effects of 5-substituted 2'-deoxyuridines on murine MO cells transformation by Moloney murine sarcoma virus.
      Proceedings of the Thirteenth International Congress of Chemotherapy, (held in Vienna, Austria, on 28 August-2 Septem­ber, 1983), K.H. Spitzy & K. Karrer (eds.).
      Verlag H. Egermann, Vienna, PS 12.4.11; part 286, pp. 24-28 (1983).
      


2393. De Clercq, E. & Balzarini, J.
      5-Ethyl-2'-deoxyuridine derivatives potentiate the cytotoxicity of cytosine arabinoside analogs for murine leukemia L1210 cells.
      Proceedings of the Thirteenth International Congress of Chemotherapy, (held in Vienna, Austria, on 28 August-2 Septem­ber, 1983), K.H. Spitzy & K. Karrer (eds.).
      Verlag H. Egermann, Vienna, PS 12.4.11; part 286, pp. 4-7 (1983).
      


2394. De Clercq, E.
      A review of the new antiherpes agents.
      Proceedings of the Thirteenth International Congress of Chemotherapy, (held in Vienna, Austria, on 28 August-2 Septem­ber, 1983), K.H. Spitzy & K. Karrer (eds.).
      Verlag H. Egermann, Vienna, SS 4.7/2; part 39, pp. 1-5 (1983).
      


2395. Bubley, G., Crumpacker, C., De Clercq, E. & Schnipper, L.
      Effects of (E)-5-(2-bromovinyl)-2'-deoxyuridine on the proli­feration of herpes sim­plex virus type 1-transformed and thymi­dine kinase-deficient mouse cells.
      Virology, 129: 490-492 (1983).
      


2396. Balzarini, J., De Clercq, E. & Dann, O.
      Inhibitory activity of diarylamidine derivatives on murine leukemia L1210 cell growth.
      Investigational New Drugs, 1: 103-115 (1983).
      


2397. De Clercq, E.
      Antivirale chemotherapie.
      In "Medische Virologie" (derde, herziene druk), red. J.B. Wil­terdink.
      Bohn, Scheltema & Holkema, Utrecht, pp. 265-285 (1983).
      


2398. De Clercq, E.
      The chemotherapy of herpesvirus infections with reference to bromovinyldeoxyuridine and other antiviral compounds.
      In "Problems of Antiviral Therapy" (Proceedings of the Fifth Beecham Colloquium on Antiviral Therapy, London, England, September 15-17, 1982), Sir Charles H. Stuart-Harris & J. Oxford (eds.).
      Academic Press, Inc., London, pp. 295-315 (1983).
      


2399. De Clercq, E.
      Selective antiherpes drugs.
      In "Medical Virology, II" (Proceedings of the International Symposium on Medical Virology, Anaheim, California, USA, Decem­ber 2-4, 1982), L.M. de la Maza & E.M. Paterson (eds.).
      Elsevier Science Publishing Co., New York, pp. 307-346 (1983).
      


2400. De Clercq, E.
      Antiviral activity of 5-substituted pyrimidine nucleoside ana­logues.
      Pure and Appl. Chem., 55: 623-636 (1983).
      


2401. Babiuk, L.A., Acres, S.D., Misra, V., Stockdale, P.H.G. & De Clercq, E.
      Susceptibility of bovid herpesvirus 1 to antiviral drugs : in vitro versus in vivo efficacy of (E)-5-(2-bromovinyl)-2'-de­oxyuridine.
      Antimicrob. Agents Chemother., 23: 715-720 (1983).
      


2402. Wang, X., Lescott, T., De Clercq, E. & Kelly, D.C.
      Baculovirus replication : inhibition of Trichoplusia ni mul­tiple nuclear polyhedrosis virus by (E)-5-(2-bromovinyl)-2'-de­oxyuridine.
      J. Gen. Virol., 64: 1221-1227 (1983).
      


2403. De Clercq, E., Descamps, J., Balzarini, J., Fukui, T. & Al­laudeen, H.S.
      Antiviral activity of the 3'-amino derivative of (E)-5-(2-bro­movinyl)-2'-deoxyuridine.
      Biochem. J., 211: 439-445 (1983).
      


2404. Cassiman, J.J., De Clercq, E. & Van den Berghe, H.
      Induction of sister chromatid exchange by 5-substituted 2'-de­oxyuridines.
      Mutation Res., 117: 317-327 (1983).
      


2405. Huygen, K., Zhang, Z.-X. & De Clercq, E.
      Failure of athymic-nude mice sensitized with Bacillus Calmette-Guérin to produce interferon in response to purified protein derivative.
      Proc. Soc. Exp. Biol. Med., 172: 260-264 (1983).
      


2406. Bussereau, F., Chermann, J.-C., De Clercq, E. & Hannoun, C.
      Search for compounds with an inhibitory effect on rhabdovirus multiplication in vitro.
      Ann. Virol., 134: 127-134 (1983).
      


2407. Bobst, A.M., Ozinskas, A.J. & De Clercq, E.
      Synthesis and biological activities of C(5)-N-spin-labeled uridines and related deriva­tives.
      Helv. Chim. Acta, 66: 534-541 (1983).
      


2408. De Clercq, E. & Montgomery, J.A.
      Broad-spectrum antiviral activity of the carbocyclic analog of 3-deazaadenosine.
      Antiviral Res., 3: 17-24 (1983).
      


2409. Park, N.-H., Pavan-Langston, D. & De Clercq, E.
      Efficacy of (E)-5-(2-bromovinyl)-2'-deoxyuridine in the treat­ment of experimental herpes simplex virus encephalitis in mice.
      Antiviral Res., 3: 7-15 (1983).
      


2410. De Clercq, E., Descamps, J., Balzarini, J., Giziewicz, J., Barr, P.J. & Robins, M.J.
      Nucleic acid related compounds. 40. Synthesis and biological activities of 5-alkynyl­uracil nucleosides.
      J. Med. Chem., 26: 661-666 (1983).
      


2411. Shigeta, S., Yokota, T., Iwabuchi, T., Baba, M., Konno, K., Ogata, M. & De Clercq, E.
      Comparative efficacy of antiherpes drugs against various strains of varicella-zoster virus.
      J. Infect. Dis., 147: 576-584 (1983).
      


2412. Colla, L., De Clercq, E., Busson, R. & Vanderhaeghe, H.
      Synthesis and antiviral activity of water-soluble esters of acyclovir [9-(2-hy­droxyethoxymethyl)guanine].
      J. Med. Chem., 26: 602-604 (1983).
      


2413. Votruba, I., Holý, A. & De Clercq, E.
      Metabolism of the broad-spectrum antiviral agent, 9-(S)-(2,3-dihydroxypro­pyl)adenine, in different cell lines.
      Acta Virol., 27: 273-276 (1983).
      


2414. Mincher, D.J., Shaw, G. & De Clercq, E.
      Anthracyclinones. Part 1. A versatile synthesis of the anthra­cyclinone system using a chiral template derived from a carbo­hydrate.
      J. Chem. Soc. Perkin Trans. I, 613-618 (1983).
      


2415. Mancini, W.R., De Clercq, E. & Prusoff, W.H.
      The relationship between incorporation of E-5-(2-bromovinyl)-2'-deoxyuridine into herpes simplex virus type 1 DNA with virus infectivity and DNA integrity.
      J. Biol. Chem., 258: 792-795 (1983).
      


2416. Balzarini, J. & De Clercq, E.
      Role of deoxycytidine kinase in the inhibitory activity of 5-substituted 2'-deoxy­cytidines and cytosine arabinosides on tu­mor cell growth.
      Mol. Pharmacol., 23: 175-181 (1983).
      



46 publications in the year 1982



2417. Holý, A., Votruba, I. & De Clercq, E.
      S-Adenosyl-L-homocysteine hydrolase and antiviral activity : structure-activity rela­tionship in the series of aliphatic nu­cleoside analogues.
      In "Metabolism and Enzymology of Nucleic Acids" (Proceedings of the Fourth Inter­national Symposium on Metabolism and Enzy­mology of Nucleic Acids, Smolenice, Czechoslovakia, 8-11 June, 1981), J. Zelinka & J. Balan (eds.).
      Publishing House of the Slovak Academy of Sciences, Bratislava, pp. 111-118 (1982).
      


2418. Fiers, W., Degrave, W., Derynck, R., Devos, R., Gheysen, D., Remaut, E., Stanssens, P., Tavernier, J., Content, J. & De Clercq, E.
      The human fibroblast interferon gene(s) and their expression in heterologous cells.
      In "Primary and Tertiary Structure of Nucleic Acids and Cancer Research", M. Miwa et al. (eds.).
      Japan Sci. Soc. Press, Tokyo, pp. 227-236 (1982).
      


2419. Colla, L., Busson, R., De Clercq, E. & Vanderhaeghe, H.
      Synthesis of aliphatic nucleoside analogues with potential an­tiviral activity.
      Eur. J. Med. Chem., 17: 569-576 (1982).
      


2420. De Clercq, E.
      Selective antiherpes agents.
      Trends in Pharmacological Sciences, 3: 492-495 (1982).
      


2421. Walker, R.T., Balzarini, J., Coe, P.L., De Clercq, E., Harnden, M.R., Jones, A.S., Noble, S.A. & Rahim, S.G.
      The synthesis and properties of some 5-substituted pyrimidine derivatives of potential biological interest.
      Nucleic Acids Res., Symposium Series no. 11: 215-218 (1982).
      


2422. De Clercq, E.
      Design of nucleoside, oligonucleotide and polynucleotide ana­logues as antiviral agents.
      Nucleic Acids Res., Symposium Series no. 11: 203-206 (1982).
      


2423. Content, J., De Wit, L., Derynck, R., De Clercq, E. & Fiers, W.
      In vitro cotranslational processing of human pre-interferon ß1 enhances its biological activity.
      Virology, 122: 466-470 (1982).
      


2424. Balzarini, J., De Clercq, E., Mertes, M.P., Shugar, D. & Tor­rence, P.F.
      5-Substituted 2'-deoxyuridines : correlation between inhibition of tumor cell growth and inhibition of thymidine kinase and thymidylate synthetase.
      Biochem. Pharmacol., 22: 3673-3682 (1982).
      


2425. Fukui, T., De Clercq, E., Kakiuchi, N. & Ikehara, M.
      Template activity of poly-(2'-fluoro-2'-deoxyinosinic acid) for murine leukemia virus reverse transcriptase.
      Cancer Letters, 16: 129-135 (1982).
      


2426. Descamps, J., Sehgal, R.K., De Clercq, E. & Allaudeen, H.S.
      Inhibitory effect of E-5-(2-bromovinyl)-1-ß-D-arabinofuranosyl­uracil on herpes sim­plex virus replication and DNA synthesis.
      J. Virol., 43: 332-336 (1982).
      


2427. De Clercq, E., Zhang, Z.-X., Huygen, K. & Leyten, R.
      Inhibitory effect of interferon on the growth of spontaneous mammary tumors in mice.
      J. Nat. Cancer Inst., 69: 653-657 (1982).
      


2428. Shigeta, S., Yokota, T., Ogata, M., Abe, K. & De Clercq, E.
      Comparative efficacy of antiherpes drugs against different strains of varicella-zoster virus.
      In "Herpesvirus : Clinical, Pharmacological and Basic Aspects" (Proceedings of an International Symposium, held in Tokushima City, Japan, on 27-30 July, 1981), H. Shiota, Y.-C. Cheng & W.H. Prusoff (eds.). Excerpta Medica (Amsterdam), pp. 94-97 (1982).
      


2429. Weinmaster, G.A., Misra, V., McGuire, R., Babiuk, L.A. & De Clercq, E.
      Bovid herpes virus type-1 (infectious bovine rhinotracheitis virus)-induced thymidine kinase.
      Virology, 118: 191-201 (1982).
      


2430. De Clercq, E.
      Specific targets for antiviral drugs.
      Biochem. J., 205: 1-13 (1982).
      


2431. Rahim, S.G., Duggan, M.J.H., Walker, R.T., Jones, A.S., Dyer, R.L., Balzarini, J. & De Clercq, E.
      Synthesis and biological properties of 2'-deoxy-5-vinyluridine and 2'-deoxy-5-vinyl­cytidine.
      Nucleic Acids Res., 10: 5285-5295 (1982).
      


2432. Balzarini, J. & De Clercq, E.
      Structure-function relationship of the antitumor cell activity of pyrimidine and pyri­dine derivatives.
      Proceedings of the 4th International Round Table on Nucleo­sides, Nucleotides and their Biological Applications (held in Antwerp, Belgium, on 4-6 February, 1981), F.C. Alderweireldt & E.L. Esmans (eds.), The University of Antwerp (R.U.C.A.), pp. 275-291 (1982).
      


2433. De Clercq, E.
      Antiviral activity of pyrimidine nucleoside analogs : a struc­ture-function analysis.
      Proceedings of the 4th International Round Table on Nucleo­sides, Nucleotides and their Biological Applications (held in Antwerp, Belgium, on 4-6 February, 1981), F.C. Alderweireldt & E.L. Esmans (eds.), The University of Antwerp (R.U.C.A.), pp. 25-45 (1982).
      


2434. Shigeta, S., Yokota, T., Takami, Z., Konno, K., Iwabuchi, T., Baba, M., Ogata, M., Suzuki, H., Nagao, S. & De Clercq, E.
      Comparative efficacy of different antiherpes drugs against dif­ferent strains of varicella-zoster virus (in Japanese).
      Jap. Med. J., 30: 23-28 (1982).
      


2435. De Clercq, E., Zhang, Z.-X. & Sim, I.S.
      Treatment of experimental herpes simplex virus encephalitis with (E)-5-(2-bromovi­nyl)-2'-deoxyuridine.
      Antimicrob. Agents Chemother., 22: 421-425 (1982).
      


2436. Balzarini, J. & De Clercq, E.
      Role of thymidine kinase in the inhibitory activity of 5-sub­stituted 2'-deoxyuridines on the growth of murine leukemia cell lines.
      In "Current Chemotherapy and Immunotherapy" (Proceedings of the Twelfth Interna­tional Congress of Chemotherapy, Florence, Italy, 19-24 July 1981), P. Periti & G.G. Grassi (eds.).
      American Society for Microbiology, Washington, D.C., pp. 1316-1319 (1982).
      


2437. Marmer, D.J., Steele, R.W. & De Clercq, E.
      Comparative in vitro immunotoxicology of (E)-5-(2-bro­movinyl)-2'-deoxyuridine and other antiviral agents.
      In "Current Chemotherapy and Immunotherapy" (Proceedings of the Twelfth Interna­tional Congress of Chemotherapy, Florence, Italy, 19-24 July 1981), P. Periti & G.G. Grassi (eds.).
      American Society for Microbiology, Washington, D.C., pp. 1065-1066 (1982).
      


2438. De Clercq, E., Busson, R., Colla, L., Descamps, J., Balzarini, J. & Vanderhaeghe, H.
      Antiviral activity of sugar-modified derivatives of (E)-5-(2-bromovinyl)-2'-deoxyuridine.
      In "Current Chemotherapy and Immunotherapy" (Proceedings of the Twelfth Interna­tional Congress of Chemotherapy, Florence, Italy, 19-24 July 1981), P. Periti & G.G. Grassi (eds.).
      American Society for Microbiology, Washington, D.C., pp. 1062-1064 (1982).
      


2439. De Clercq, E., Whitley, R.J., Helgstrand, E., Keeney, R.E., Crumpacker, C., Young, C.W., Kern, E.R. & Galasso, G.J.
      Antiherpes chemotherapy.
      In "Current Chemotherapy and Immunotherapy" (Proceedings of the Twelfth Interna­tional Congress of Chemotherapy, Florence, Italy, 19-24 July 1981), P. Periti & G.G. Grassi (eds.).
      American Society for Microbiology, Washington, D.C., pp. 1053-1059 (1982).
      


2440. De Clercq, E. & Torrence, P.F.
      Structure-activity relationships for interferon induction and inhibition of protein syn­thesis by polynucleotides.
      Texas Reports on Biology and Medicine, 41: 76-83 (1982).
      


2441. Zhang, Z.-X., De Clercq, E., Heremans, H., Verhaegen-Lewalle, M. & Content, J.
      Antiviral and anticellular activities of human and murine type I and type II interferons in human cells monosomic, disomic, and trisomic for chromosome 21.
      Proc. Soc. Exp. Biol. Med., 170: 103-111 (1982).
      


2442. Wigdahl, B.L., Scheck, A.C., De Clercq, E. & Rapp, F.
      High efficiency latency and activation of herpes simplex virus in human cells.
      Science, 217: 1145-1146 (1982).
      


2443. Maudgal, P.C., Uyttebroeck, W., De Clercq, E. & Missotten, L.
      Oral and topical treatment of experimental herpes simplex iri­tis with bromovinylde­oxyuridine.
      Arch. Ophthalmol., 100: 1337-1340 (1982).
      


2444. De Clercq, E.
      Interferon : a molecule for all seasons.
      In "Virus Infections : Modern Concepts and Status", L.C. Olson (ed.).
      Marcel Dekker, Inc., New York, pp. 87-138 (1982).
      


2445. Fukui, T. & De Clercq, E.
      Inhibition of murine leukaemia virus reverse transcriptase by 2-halogenated poly­adenylic acids.
      Biochem. J., 203: 755-760 (1982).
      


2446. Park, N.-H., Pavan-Langston, D. & De Clercq, E.
      Effects of acyclovir, bromovinyldeoxyuridine, vidarabine and L-lysine on latent gan­glionic herpes simplex virus in vitro.
      Am. J. Med., 73: 151-154 (1982).
      


2447. Park, N.-H., Pavan-Langston, D., Boisjoly, H.M. & De Clercq, E.
      Chemotherapeutic efficacy of E-5-(2-bromovinyl)-2'-deoxyuridine for orofacial infec­tion with herpes simplex virus type 1 in mice.
      J. Infect. Dis., 145: 909-913 (1982).
      


2448. Maudgal, P.C., De Kimpe, N., De Clercq, E., Descamps, J., Mis­sotten, L. & Geysen, A.
      Influence of (E)-5-(2-bromovinyl)-2'-deoxyuridine on corneal epithelium healing.
      Graefe's Arch. Clin. Exp. Ophthalmol., 218: 275-281 (1982).
      


2449. De Clercq, E., Zhang, Z.-X. & Huygen, K.
      Synergism in the antitumor effects of type I and type II inter­feron in mice inoculated with leukemia L1210 cells.
      Cancer Letters, 15: 223-228 (1982).
      


2450. Content, J., De Wit, L., Piérard, D., Derynck, R., De Clercq, E. & Fiers, W.
      Secretory proteins induced in human fibroblasts under condi­tions used for the pro­duction of interferon ß.
      Proc. Nat. Acad. Sci. USA, 79: 2768-2772 (1982).
      


2451. De Clercq, E.
      Comparative efficacy of antiherpes drugs in different cell lines.
      Antimicrob. Agents Chemother., 21: 661-663 (1982).
      


2452. Holý, A., Votruba, I. & De Clercq, E.
      Synthesis and antiviral activity of stereoisomeric eritadenines.
      Collect. Czech. Chem. Commun., 47: 1392-1407 (1982).
      


2453. Verhaegen-Lewalle, M., Kuwata, T., Zhang, Z.-X., De Clercq, E., Cantell, K. & Content, J.
      2-5A Synthetase activity induced by interferon , ß and  in human cell lines differing in their sensitivity to the anticel­lular and antiviral activities of these interferons.
      Virology, 117: 425-434 (1982).
      


2454. De Clercq, E. & Zhang, Z.-X.
      Differential effects of (E)-5-(2-bromovinyl)-2'-deoxyuridine on infections with herpes simplex virus type 1 and type 2 in hair­less mice.
      J. Infect. Dis., 145: 130 (1982).
      


2455. Maudgal, P.C., De Clercq, E., Descamps, J., Missotten, L. & Wijnhoven, J.
      Experimental stromal herpes simplex keratitis. Influence of treatment with topical bromovinyldeoxyuridine and trifluridine.
      Arch. Ophthalmol., 100: 653-656 (1982).
      


2456. Balzarini, J., De Clercq, E., Torrence, P.F., Mertes, M.P., Park, J.S., Schmidt, C.L., Shugar, D., Barr, P.J., Jones, A.S., Verhelst, G. & Walker, R.T.
      Role of thymidine kinase in the inhibitory activity of 5-sub­stituted 2'-deoxyuridines on the growth of human and murine tu­mor cell lines.
      Biochem. Pharmacol., 31: 1089-1095 (1982).
      


2457. Kakiuchi, N., Marck, C., Rousseau, N., Leng, M., De Clercq, E. & Guschlbauer, W.
      Polynucleotide helix geometry and stability : spectroscopic, antigenic and interferon-inducing properties of deoxyribose-, ribose-, or 2'-deoxy-2'-fluororibose-containing duplexes of poly(inosinic acid).poly(cytidylic acid).
      J. Biol. Chem., 257: 1924-1928 (1982).
      


2458. De Clercq, E., Balzarini, J., Descamps, J., Huang, G.-F., Tor­rence, P.F., Bergstrom, D.E., Jones, A.S., Serafinowski, P., Verhelst, G. & Walker, R.T.
      Antiviral, antimetabolic, and cytotoxic activities of 5-substi­tuted 2'-deoxycytidines.
      Mol. Pharmacol., 21: 217-223 (1982).
      


2459. Allaudeen, H.S., Chen, M.S., Lee, J.J., De Clercq, E. & Pru­soff, W.H.
      Incorporation of E-5-(2-halovinyl)-2'-deoxyuridines into de­oxyribonucleic acids of herpes simplex virus type 1-infected cells.
      J. Biol. Chem., 257: 603-606 (1982).
      


2460. De Clercq, E.
      Effects of interferon on human tumor cell growth in nude mice.
      In "The Nude Mouse in Experimental and Clinical Research", Vol. 2, J. Fogh & B.C. Giovanella (eds.). Academic Press, Inc., New York, pp. 439-449 (1982).
      


2461. Wigdahl, B.L., Isom, H.C., De Clercq, E. & Rapp, F.
      Activation of herpes simplex virus (HSV) type 1 genome by tem­perature-sensitive mutants of HSV type 2.
      Virology, 116: 468-479 (1982).
      


2462. De Clercq, E., Descamps, J., Ogata, M. & Shigeta, S.
      In vitro susceptibility of varicella-zoster virus to E-5(-2-bromovinyl)-2'-deoxyuridine and related compounds.
      Antimicrob. Agents Chemother., 21: 33-38 (1982).
      



38 publications in the year 1981



2463. Derynck, R., Devos, R., Remaut, E., Saman, E., Stanssens, P., Tavernier, J., Volckaert, G., Content, J., De Clercq, E. & Fiers, W.
      Isolation and characterization of a human fibroblast interferon gene and its expression in Escherichia coli.
      Reviews of Infectious Diseases, 3: 1186-1195 (1981).
      


2464. Maudgal, P.C., Dralands, L., Lamberts, L., De Clercq, E., Descamps, J. & Missotten, L.
      Preliminary results of oral BVDU treatment of herpes zoster ophthalmicus.
      Bull. Soc. Belge Ophtalmol., 193: 49-56 (1981).
      


2465. Hettinger, M.E., Pavan-Langston, D., Park, N.-H., Albert, D.M., De Clercq, E. & Lin, T.-S.
      Ac2IDU, BVDU, and thymine arabinoside therapy in experimental herpes keratitis.
      Arch. Ophthalmol., 99: 1618-1621 (1981).
      


2466. Bobst, A.M., Langemeier, P.W., Torrence, P.F. & De Clercq, E.
      Interferon induction by poly(inosinic acid).poly(cytidylic acid) segmented by spin-labels.
      Biochemistry, 20: 4798-4803 (1981).
      


2467. Baglioni, C., Minks, M.A. & De Clercq, E.
      Structural requirements of polynucleotides for the activation of (2'-5')An polymerase and protein kinase.
      Nucleic Acids Res., 9: 4939-4950 (1981).
      


2468. De Clercq, E., Verhelst, G., Descamps, J. & Bergstrom, D.E.
      Differential inhibition of herpes simplex viruses, type 1 (HSV-1) and type 2 (HSV-2), by (E)-5-(2-X-vinyl)-2'-deoxyuridines.
      Acta Microbiol. Acad. Sci. Hung., 28: 307-312 (1981).
      


2469. De Clercq, E.
      Nucleoside analogues as antiviral agents.
      Acta Microbiol. Acad. Sci. Hung., 28: 289-306 (1981).
      


2470. Content, J., De Wit, L., Johnston, M.I. & De Clercq, E.
      Procedures for the measurement of interferon mRNA distribution in induced mouse cells.
      In "Methods in Enzymology", S.P. Colowick & N.O. Kaplan (eds.). Volume 78, "Interferons", S. Pestka (ed.).
      Academic Press, Inc., (New York), Part B, pp. 125-131 (1981).
      


2471. Torrence, P.F. & De Clercq, E.
      Interferon inducers : general survey and classification.
      In "Methods in Enzymology", S.P. Colowick & N.O. Kaplan (eds.). Volume 78, "Interferons", S. Pestka (ed.).
      Academic Press, Inc., (New York), Part A, pp. 291-299 (1981).
      


2472. De Clercq, E.
      Interferon induction by polynucleotides, modified polynu­cleotides and polycarboxy­lates.
      In "Methods in Enzymology", S.P. Colowick & N.O. Kaplan (eds.). Volume 78, "Interferons", S. Pestka (ed.).
      Academic Press, Inc., (New York), Part A, pp. 227-236 (1981).
      


2473. Field, H.J. & De Clercq, E.
      Effects of oral treatment with acyclovir and bro­movinyldeoxyuridine on the establishment and maintenance of la­tent herpes simplex virus infection in mice.
      J. Gen. Virol., 56: 259-265 (1981).
      


2474. De Clercq, E.
      Antivirale werking van nucleoside analoga.
      Tijdschr. Geneesk., 37: 1045-1057 (1981).
      


2475. Cassiman, J.J., De Clercq, E., Jones, A.S., Walker, R.T. & Van den Berghe, H.
      Sister chromatid exchange induced by anti-herpes drugs.
      Brit. Med. J., 283: 817-818 (1981).
      


2476. Kulikowski, T., Zawadzki, Z., Shugar, D. & De Clercq, E.
      Pyrimidine arabinofuranosyl nucleosides with 5-substituted long-branched and unsatu­rated chains : synthesis and antiherpes properties.
      Nucleic Acids Res., Symposium Series no. 9: 103-106 (1981).
      


2477. Busson, R., Colla, L., Vanderhaeghe, H. & De Clercq, E.
      Synthesis and antiviral activity of some sugar-modified deriva­tives of (E)-5-(2-bro­movinyl)-2'-deoxyuridine.
      Nucleic Acids Res., Symposium Series no. 9: 49-52 (1981).
      


2478. Walker, R.T., Jones, A.S., Rahim, S.G., Serafinowski, P. & De Clercq, E.
      The synthesis and properties of some 5-substituted uracil derivatives.
      Nucleic Acids Res., Symposium Series no. 9: 21-24 (1981).
      


2479. De Clercq, E., Zhang, Z.-X. & Huygen, K.
      Antiviral potentials of interferon as opposed to other antivi­ral agents.
      In "The Biology of the Interferon System", E. De Maeyer, G. Galasso & H. Schellekens (eds.). Elsevier/North-Holland Biome­dical Press, Amsterdam, pp. 375-380 (1981).
      


2480. Huygen, K., Zhang, Z.-X., De Clercq, E. & Palfliet, K.
      Anticellular and antiviral effects of semi-purified murine gamma-interferon.
      In "The Biology of the Interferon System", E. De Maeyer, G. Galasso & H. Schellekens (eds.). Elsevier/North-Holland Biome­dical Press, Amsterdam, pp. 307-311 (1981).
      


2481. Cheng, Y.-C., Dutschman, G., De Clercq, E., Jones, A.S., Rahim, S.G., Verhelst, G. & Walker, R.T.
      Differential affinities of 5-(2-halogenovinyl)-2'-deoxyuridines for deoxythymidine kinases of various origins.
      Mol. Pharmacol., 20: 230-233 (1981).
      


2482. Chandra, P., Demirhan, I. & De Clercq, E.
      A study of antitemplate inhibition of mammalian, bacterial and viral DNA po­lymerases by 2- and 2'-substituted derivatives of polyadenylic acid.
      Cancer Letters, 12: 181-193 (1981).
      


2483. De Clercq, E.
      Therapeutic potentials of BVDU [E-5-(2-bromovinyl)-2'-deoxyuridine] as an antiher­pes drug.
      Chemioterapia Antimicrobica, 4: 70-75 (1981).
      


2484. Descamps, J. & De Clercq, E.
      Specific phosphorylation of E-5-(2-iodovinyl)-2'-deoxyuridine by herpes simplex virus-infected cells.
      J. Biol. Chem., 256: 5973-5976 (1981).
      


2485. De Clercq, E., Leyten, R., Sobis, H., Matousek, J., Holý, A. & De Somer, P.
      Inhibitory effect of a broad-spectrum antiviral agent, (S)-9-(2,3-dihydroxypropyl)-adenine, on spermatogenesis in mice.
      Toxicol. Appl. Pharmacol., 59: 441-451 (1981).
      


2486. Allaudeen, H.S., Kozarich, J.W., Bertino, J.R. & De Clercq, E.
      On the mechanism of selective inhibition of herpesvirus repli­cation by (E)-5-(2-bro­movinyl)-2'-deoxyuridine.
      Proc. Nat. Acad. Sci. USA, 78: 2698-2702 (1981).
      


2487. De Clercq, E., Zhang, Z.-X., Descamps, J. & Huygen, K.
      E-5-(2-Bromovinyl)-2'-deoxyuridine vs. interferon in the sys­temic treatment of herpes simplex virus infection of athymic nude mice.
      J. Infect. Dis., 143: 846-852 (1981).
      


2488. Allaudeen, H.S., Kozarich, J.W., Bertino, J.R. & De Clercq, E.
      A biochemical mechanism for selective inhibition of herpesvirus replication by (E)-5-(2-bromovinyl)-2'-deoxyuridine.
      In "Antiviral Chemotherapy : Design of Inhibitors of Viral Functions" (Proceedings of the Second International Symposium on Antiviral Chemotherapy, Hamburg, 27-29 August, 1980), K.K. Gauri (ed.).
      Academic Press, Inc. (New York), pp. 89-98 (1981).
      


2489. De Clercq, E.
      Interferon Anno 1980.
      In "Antiviral Chemotherapy : Design of Inhibitors of Viral Functions" (Proceedings of the Second International Symposium on Antiviral Chemotherapy, Hamburg, 27-29 August, 1980), K.K. Gauri (ed.).
      Academic Press, Inc. (New York), pp. 279-298 (1981).
      


2490. Jones, A.S., Rahim, S.G., Walker, R.T. & De Clercq, E.
      Synthesis and antiviral properties of (Z)-5-(2-bromovinyl)-2'-deoxyuridine.
      J. Med. Chem., 24: 759-760 (1981).
      


2491. Huang, G.-F., Okada, M., De Clercq, E. & Torrence, P.F.
      Synthesis and antiviral activity of 5-[(cyanomethylene)oxy]-2'-deoxyuridine.
      J. Med. Chem., 24: 390-393 (1981).
      


2492. Vandenbussche, P., Divizia, M., Verhaegen-Lewalle, M., Fuse, A., Kuwata, T., De Clercq, E. & Content, J.
      Enzymatic activities induced by interferon in human fibroblast cell lines differing in their sensitivity to the anticellular activity of interferon.
      Virology, 111: 11-22 (1981).
      


2493. Maudgal, P.C., Missotten, L., De Clercq, E., Descamps, J. & De Meuter, E.
      Efficacy of (E)-5-(2-bromovinyl)-2'-deoxyuridine in the topical treatment of herpes simplex keratitis.
      Albrecht von Graefes Arch. Klin. Ophthalmol., 216: 261-268 (1981).
      


2494. Maudgal, P.C., De Clercq, E., Descamps, J. & Missotten, L.
      Efficacy of E-5-(2-bromovinyl)-2'-deoxyuridine in the topical treatment of herpetic keratitis in rabbits and man.
      In "Herpetic Eye Diseases" (Proceedings of the International Symposium of the Ger­man Ophthalmologic Society on Herpetic Eye Diseases, held in Freiburg im Breisgau, 12-14 April 1980), R. Sundmacher (ed.).
      J.F. Bergmann-Verlag (München), pp. 339-341 (1981).
      


2495. De Clercq, E. & Descamps, J.
      On the mechanism of anti-herpes action of E-5-(2-bromovinyl)-2'-deoxyuridine.
      In "Herpetic Eye Diseases" (Proceedings of the International Symposium of the Ger­man Ophthalmologic Society on Herpetic Eye Diseases, held in Freiburg im Breisgau, 12-14 April 1980), R. Sundmacher (ed.).
      J.F. Bergmann-Verlag (München), pp. 329-338 (1981).
      


2496. De Clercq, E.
      Genetische manipulatie en interferon.
      Onze Alma Mater (Driemaandelijks Tijdschrift van Vlaamse Leer­gangen te Leuven), 35: 19-49 (1981).
      


2497. De Clercq, E.
      Interferon.
      Belgian Medical Year Book 1981 : 194-199 (1981).
      


2498. De Clercq, E., Balzarini, J., Torrence, P.F., Mertes, M.P., Schmidt, C.L., Shugar, D., Barr, P.J., Jones, A.S., Verhelst, G. & Walker, R.T.
      Thymidylate synthetase as target enzyme for the inhibitory ac­tivity of 5-substituted 2'-deoxyuridines on mouse leukemia L-1210 cell growth.
      Mol. Pharmacol., 19: 321-330 (1981).
      


2499. De Clercq, E., Heremans, H., Descamps, J., Verhelst, G., De Ley, M. & Billiau, A.
      Effects of E-5-(2-bromovinyl)-2'-deoxyuridine and other selec­tive anti-herpes com­pounds on the induction of retrovirus parti­cles in mouse BALB/3T3 cells.
      Mol. Pharmacol., 19: 122-129 (1981).
      


2500. De Clercq, E., Balzarini, J., Descamps, J., Bigge, C.F., Chang, C.T.-C., Kalaritis, P. & Mertes, M.P.
      Antiviral, antitumor, and thymidylate synthetase inhibition studies of 5-substituted styryl derivatives of 2'-deoxyuridine and their 5'-phosphates.
      Biochem. Pharmacol., 30: 495-502 (1981).
      



29 publications in the year 1980



2501. Maudgal, P.C., Missotten, L., De Clercq, E. & Descamps, J.
      Varicella zoster virus in the human corneal endothelium : a case report.
      Bull. Soc. Belge Ophtal., 190: 71-86 (1980).
      


2502. De Clercq, E., Balzarini, J., Chang, C.T.-C., Bigge, C.F., Kalaritis, P. & Mertes, M.P.
      5(E)-(3-Azidostyryl)-2'-deoxyuridine 5'-phosphate is a photoac­tivated inhibitor of thymidylate synthetase.
      Biochem. Biophys. Res. Commun., 97: 1068-1075 (1980).
      


2503. Johnston, M.I., Zoon, K.C., Friedman, R.M., De Clercq, E. & Torrence, P.F.
      Oligo(2'-5')adenylate synthetase activity in human lymphoblas­toid cells.
      Biochem. Biophys. Res. Commun., 97: 375-383 (1980).
      


2504. De Clercq, E., Descamps, J., Maudgal, P.C., Missotten, L., Leyten, R., Verhelst, G., Jones, A.S., Walker, R.T., Busson, R., Vanderhaeghe, H. & De Somer, P.
      Selective anti-herpes activity of 5-(2-halogenovinyl)-2'-de­oxyuridines and 2'-deoxy­cytidines.
      In "Developments in Antiviral Therapy", L.H. Collier & J. Ox­ford (eds.). Academic Press, Inc., London, pp. 21-42 (1980).
      


2505. Holý, A. & De Clercq, E.
      Preparation, spectral properties and biological activities of 5-bromo-6-methyl-2'-deoxy­uridine and 5-iodo-6-methyl-2'-de­oxyuridine.
      Collect. Czech. Chem. Commun., 45: 2364-2370 (1980).
      


2506. Braude, I.A., De Clercq, E., Zhang, Z.-X., Edy, V.G. & De Somer, P.
      Neutralization of interferon activity in homologous and he­terologous cells with homologous and heterologous antibody.
      Proc. Soc. Exp. Biol. Med., 165: 161-166 (1980).
      


2507. De Clercq, E., Degreef, H., Wildiers, J., De Jonge, G., Drochmans, A., Descamps, J. & De Somer, P.
      Oral (E)-5-(2-bromovinyl)-2'-deoxyuridine in severe herpes zoster infections.
      Brit. Med. J., 281: 1178 (1980).
      


2508. De Clercq, E., Descamps, J., De Somer, P., Samyn, C. & Smets, G.
      Alopecia in laboratory animals induced by a polyampholyte, polyethylene alanine.
      Experientia, 36: 1107-1108 (1980).
      


2509. Derynck, R., Remaut, E., Saman, E., Stanssens, P., De Clercq, E., Content, J. & Fiers, W.
      Expression of the human fibroblast interferon gene in Escherichia coli.
      Nature, 287: 193-197 (1980).
      


2510. Derynck, R., Content, J., De Clercq, E., Volckaert, G., Ta­vernier, J., Devos, R. & Fiers, W.
      Isolation and structure of a human fibroblast interferon gene.
      Nature, 285: 542-547 (1980).
      


2511. Walker, R.T., Jones, A.S., De Clercq, E., Descamps, J., Al­laudeen, H.S. & Kozarich, J.W.
      The synthesis and properties of some 5-substituted uracil derivatives.
      Nucleic Acids Res., Symposium Series, no. 8: s95-s102 (1980).
      


2512. De Clercq, E.
      Antiviral and antitumor activities of 5-substituted 2'-de­oxyuridines.
      Methods and Findings in Experimental and Clinical Pharmacology, 2: 253-267 (1980).
      


2513. De Clercq, E., Kulikowski, T. & Shugar, D.
      The 5'-monophosphates of 5-propyl- and 5-ethyl-2'-deoxyuridine do not inhibit the replication of deoxythymidine kinase defi­cient (TK-) mutants of herpes simplex virus.
      Biochem. Pharmacol., 29: 2883-2885 (1980).
      


2514. Content, J., Johnston, M.I., De Wit, L., De Maeyer-Guignard, J. & De Clercq, E.
      Kinetics and distribution of interferon mRNA in interferon-primed and unprimed mouse L-929 cells.
      Biochem. Biophys. Res. Commun., 96: 415-424 (1980).
      


2515. De Clercq, E.
      Bromovinyldeoxyuridine.
      Drugs of the Future, 5: 334-336 (1980).
      


2516. De Clercq, E.
      Antivirale Chemotherapie.
      Belgian Medical Year Book 1980 : 236-243 (1980).
      


2517. De Clercq, E., Balzarini, J., Descamps, J. & Eckstein, F.
      Antiviral, antimetabolic and antineoplastic activities of 2'- or 3'-amino- or azido-substi­tuted deoxyribonucleosides.
      Biochem. Pharmacol., 29: 1849-1851 (1980).
      


2518. De Clercq, E.
      a) Nieuwe perspectieven in de chemotherapie van herpesvirus infecties.
      Ars Medici (Internationaal Tijdschrift voor Praktische Therapie), 9: 337-352 (1980).
      b) Nouvelles perspectives dans la chimiothérapie des infections à virus herpétiques.
      Ars Medici (Revue Internationale de Thérapie Pratique), 35: 649-664 (1980).
      


2519. Park, J.S., Chang, C.T.-C., Schmidt, C.L., Golander, Y., De Clercq, E., Descamps, J. & Mertes, M.P.
      Oxime and dithiolane derivatives of 5-formyl-2'-deoxyuridine and their 5'-phosphates : antiviral effects and thymidylate synthetase inhibition.
      J. Med. Chem., 23: 661-665 (1980).
      


2520. De Clercq, E. & Dann, O.
      Diaryl amidine derivatives as oncornaviral DNA polymerase in­hibitors.
      J. Med. Chem., 23: 787-795 (1980).
      


2521. Anné, J., De Clercq, E., Eyssen, H. & Dann, O.
      Antifungal and antibacterial activity of diarylamidine deriva­tives.
      Antimicrob. Agents Chemother., 18: 231-239 (1980).
      


2522. Schmidt, C.L., Chang, C.T.-C., De Clercq, E., Descamps, J. & Mertes, M.P.
      Synthesis of 5-[(methylthio)methyl]-2'-deoxyuridine, the cor­responding sulfoxide and sulfone, and their 5'-phosphates : an­tiviral effects and thymidylate synthetase inhibi­tion.
      J. Med. Chem., 23: 252-256 (1980).
      


2523. De Clercq, E., Descamps, J., Verhelst, G., Jones, A.S. & Walker, R.T.
      Antiviral activity of 5-(2-halogenovinyl)-2'-deoxyuridines.
      In "Current Chemotherapy and Infectious Disease" (Proceedings of the Eleventh Inter­national Congress of Chemotherapy-Nine­teenth Interscience Conference on Antimi­crobial Agents and Chemotherapy, Boston, Massachusetts, USA, 1-5 October, 1979), J.D. Nelson & C. Grassi (eds.).
      American Society for Microbiology, Washington, D.C., pp. 1372-1374 (1980).
      


2524. De Clercq, E.
      Interferon inducers.
      In "Virus Chemotherapy", F.E. Hahn (ed.), S. Karger AG (Basel).
      Antibiotics Chemother., 27: 251-287 (1980).
      


2525. Volckaert-Vervliet, G., De Clercq, E. & Billiau, A.
      Interaction of polyriboinosinic acid.polyribocytidylic acid with human lymphoblastoid cells.
      Biochem. Biophys. Res. Commun., 92: 833-838 (1980).
      


2526. De Clercq, E., Stollar, B.D., Hobbs, J., Fukui, T., Kakiuchi, N. &
      Interferon induction by two 2'-modified double-stranded RNAs : poly(2'-fluoro-2'-deoxyinosinic acid).poly(cytidylic acid) and poly(2'-chloro-2'-deoxyinosinic acid).poly(cytidylic acid).
      Eur. J. Biochem., 107: 279-288 (1980).
      


2527. De Clercq, E., Descamps, J., Verhelst, G., Walker, R.T., Jones, A.S., Torrence, P.F. & Shugar, D.
      Comparative efficacy of different antiherpes drugs against dif­ferent strains of herpes simplex virus.
      J. Infect. Dis., 141: 563-574 (1980).
      


2528. De Clercq, E. & De Somer, P.
      Local Shwartzman phenomenon in athymic nude mice.
      Proc. Soc. Exp. Biol. Med., 164: 75-81 (1980).
      


2529. Maudgal, P.C., De Clercq, E., Descamps, J., Missotten, L., De Somer, P., Busson, R., Vanderhaeghe, H., Verhelst, G., Walker, R.T. & Jones, A.S.
      (E)-5-(2-Bromovinyl)-2'-deoxyuridine in the treatment of expe­rimental herpes simplex keratitis.
      Antimicrob. Agents Chemother., 17: 8-12 (1980).
      



25 publications in the year 1979



2530. Maudgal, P.C., De Clercq, E., Descamps, J. & Missotten, L.
      Comparative evaluation of BVDU [(E)-5-(2-bromovinyl)-2'-de­oxyuridine] and IDU (5-iodo-2'-deoxyuridine) in the treatment of experimental herpes simplex keratitis in rabbits.
      Bull. Soc. Belge Ophtal., 186: 109-118 (1979).
      


2531. De Clercq, E., Huang, G.-F., Bhooshan, B., Ledley, G. & Tor­rence, P.F.
      Interferon induction by mismatched analogues of polyinosinic acid.polycytidylic acid [(In,U)n.(C)n].
      Nucleic Acids Res., 7: 2003-2014 (1979).
      


2532. Descamps, J., De Clercq, E., Barr, P.J., Jones, A.S., Walker, R.T., Torrence, P.F. & Shugar, D.
      Relative potencies of different anti-herpes agents in the topi­cal treatment of cutaneous herpes simplex virus infection of athymic nude mice.
      Antimicrob. Agents Chemother., 16: 680-682 (1979).
      


2533. De Clercq, E.
      Suramin : a potent inhibitor of the reverse transcriptase of RNA tumor viruses.
      Cancer Letters, 8: 9-22 (1979).
      


2534. De Clercq, E., Descamps, J., Schmidt, C.L. & Mertes, M.P.
      Antiviral activity of 5-methylthiomethyl-2'-deoxyuridine and other 5-substituted 2'-deoxyuridines.
      Biochem. Pharmacol., 28: 3249-3254 (1979).
      


2535. Braude, I.A., Edy, V.G. & De Clercq, E.
      Mechanism of binding of mouse interferon to controlled pore glass.
      Biochim. Biophys. Acta, 580: 15-23 (1979).
      


2536. Braude, I. & De Clercq, E.
      Mechanism of interaction of sodium dodecyl sulfate with mouse interferon.
      J. Biol. Chem., 254: 7758-7764 (1979).
      


2537. Braude, I.A. & De Clercq, E.
      Purification of mouse interferon by concert chromatography.
      J. Chromatogr., 172: 207-219 (1979).
      


2538. De Clercq, E., Descamps, J., De Somer, P., Barr, P.J., Jones, A.S. & Walker, R.T.
      Pharmacokinetics of E-5-(2-bromovinyl)-2'-deoxyuridine in mice.
      Antimicrob. Agents Chemother., 16: 234-236 (1979).
      


2539. Billiau, A., De Somer, P., Edy, V.G., De Clercq, E. & Heremans, H.
      Human fibroblast interferon for clinical trials : pharmacoki­netics and tolerability in experimental animals and humans.
      Antimicrob. Agents Chemother., 16: 56-63 (1979).
      


2540. De Clercq, E., Descamps, J., De Somer, P., Barr, P.J., Jones, A.S. & Walker, R.T.
      E-5-(2-Bromovinyl)-2'-deoxyuridine : a potent and selective an­tiherpes agent.
      Proc. Nat. Acad. Sci. USA, 76: 2947-2951 (1979).
      


2541. De Clercq, E.
      Antivirale Chemotherapie.
      In "Medische Virologie" (tweede, herziene druk) (red. J.B. Wil­terdink).
      Bohn, Scheltema & Holkema, Utrecht, pp. 241-265 (1979).
      


2542. De Clercq, E., Fukui, T., Kakiuchi, N., Ikehara, M., Hattori, M. & Pfleiderer, W.
      Influence of various 2- and 2'-substituted polyadenylic acids on Murine leukemia virus reverse transcriptase.
      Cancer Letters, 7: 27-37 (1979).
      


2543. De Clercq, E.
      New trends in antiviral chemotherapy.
      Arch. Intern. Physiol. Biochim., 87: 353-395 (1979).
      


2544. De Clercq, E.
      Concluding Remarks.
      "Anti-Herpesvirus Chemotherapy : Experimental and Clinical As­pects" (ed. K.K. Gauri). S. Karger AG (Basel).
      Adv. Ophthal., 38: 297-300 (1979).
      


2545. De Clercq, E.
      5-Substituted 2'-deoxyuridines which selectively inhibit herpes simplex virus replication.
      "Anti-Herpesvirus Chemotherapy : Experimental and Clinical As­pects" (ed. K.K. Gauri). S. Karger AG (Basel).
      Adv. Ophthal., 38: 204-213 (1979).
      


2546. Torrence, P.F., De Clercq, E., Descamps, J., Huang, G.-F. & Witkop, B.
      Synthesis and antiviral activities of new 5-substituted pyrimi­dine nucleoside analogs.
      In "Frontiers in Bioorganic Chemistry and Molecular Biology", Chapter IV (eds. Yu.A. Ovchinnikov & M.N. Kolosov).
      Elsevier/North-Holland Biomedical Press (Amsterdam), pp. 59-85 (1979).
      


2547. Kulikowski, T., Zawadzki, Z., Shugar, D., Descamps, J. & De Clercq, E.
      Synthesis and antiviral activities of arabinofuranosyl-5-ethylpyrimidine nucleosides. Selective anti-herpes activity of 1-(ß-D-arabinofuranosyl)-5-ethyluracil.
      J. Med. Chem., 22: 647-653 (1979).
      


2548. De Clercq, E. & Holý, A.
      Antiviral activity of aliphatic nucleoside analogues : struc­ture-function relationship.
      J. Med. Chem., 22: 510-513 (1979).
      


2549. De Clercq, E.
      Anti-herpes chemotherapie.
      Tijdschr. Geneesk., 35: 555-564 (1979).
      


2550. De Clercq, E.
      Degradation of poly(inosinic acid).poly(cytidylic acid) [(I)n.(C)n] by human plasma.
      Eur. J. Biochem., 93: 165-172 (1979).
      


2551. Torrence, P.F., Huang, G.-F., Edwards, M., Bhooshan, B., Descamps, J. & De Clercq, E.
      5-Substituted uracil arabinonucleosides as potential antiviral agents.
      J. Med. Chem., 22: 316-319 (1979).
      


2552. De Clercq, E., Descamps, J., Barr, P.J., Jones, A.S., Serafi­nowski, P., Walker, R.T., Huang, G.F., Torrence, P.F., Schmidt, C.L., Mertes, M.P., Kulikowski, T. & Shugar, D.
      Comparative study of the potency and selectivity of anti-herpes compounds.
      In "Antimetabolites in Biochemistry, Biology and Medicine", (eds. J. Skoda & P. Langen).
      Pergamon Press, Oxford and New York, pp. 275-285 (1979).
      


2553. De Clercq, E.
      Interferon induction by synthetic polynucleotides : recent de­velopments.
      In "Antiviral Mechanisms in the Control of Neoplasia" (ed. P. Chandra).
      NATO Advanced Study Institute Series; Series A - Life Sciences, Plenum Press, New York, Vol. 20, pp. 641-661 (1979).
      


2554. De Clercq, E.
      Inhibition of oncornavirus activities by polynucleotide ana­logues.
      In "Antiviral Mechanisms in the Control of Neoplasia" (ed. P. Chandra).
      NATO Advanced Study Institute Series; Series A - Life Sciences, Plenum Press, New York, Vol. 20, pp. 539-551 (1979).
      



25 publications in the year 1978



2555. Szmigielski, S., Bielec, M., Janiak, M., Kobus, M., Luczak, M. & De Clercq, E.
      Inhibition of tumor growth in mice by microwave hyperthermia, poly(I).poly(C) and mouse interferon.
      IEEE (Institute of Electrical and Electronics Engineers) Trans­actions on Microwave Theory and Techniques, Vol. MTT-26: 520-522 (1978).
      


2556. De Clercq, E., Georgiades, J.A., Edy, V.G. & Sobis, H.
      Effect of human and mouse interferon, and of polyriboinosinic acid.polyribocytidylic acid, on the growth of human fibrosar-coma and melanoma tumors in nude mice.
      Eur. J. Cancer, 14: 1273-1282 (1978).
      


2557. Mertes, M.P., Chang, C.T.-C., De Clercq, E., Huang, G.-F. & Tor­rence, P.F.
      5-Nitro-2'-deoxyuridine 5'-monophosphate is a potent irrever-sible inhibitor of Lactoba­cillus caesi thymidylate synthe-tase.
      Biochem. Biophys. Res. Commun., 84: 1054-1059 (1978).
      


2558. Walker, R.T., Barr, P.J., De Clercq, E., Descamps, J., Jones, A.S. & Serafinowski, P.
      The synthesis and properties of some antiviral nucleosides.
      Proceedings of the Fourth Symposium on the Chemistry of Nucleic Acid Components, held at Bechyne, Czechoslovakia, September 3-10, 1978.
      Nucleic Acids Res., special publication, no. 4, s103-s106 (1978).
      


2559. De Clercq, E., Torrence, P.F., Stollar, B.D., Hobbs, J., Fukui, T., Kakiuchi, N. & Ikehara, M.
      Interferon induction by a 2'-modified double-helical RNA, poly-(2'-azido-2'-deoxyinosinic acid).polycytidylic acid.
      Eur. J. Biochem., 88: 341-349 (1978).
      


2560. De Clercq, E. & Torrence, P.F.
      Nucleoside analogs with selective antiviral activity.
      J. Carbohydrates.Nucleosides.Nucleotides, 5: 187-224 (1978).
      


2561. Krajewska, E., De Clercq, E. & Shugar, D.
      Nucleoside-catabolizing enzyme activities in primary rabbit kid­ney cells and human skin fibroblasts.
      Biochem. Pharmacol., 27: 1421-1426 (1978).
      


2562. De Clercq, E., Fukui, T., Kakiuchi, N. & Ikehara, M.
      Interferon inducing activity of a 2'-modified double-stranded complex, poly(2'-azido-2'-deoxyinosinic acid).poly(cytidylic acid).
      J. Pharm. Dyn., 1: 62-65 (1978).
      


2563. Ottenheijm, H.C.J., Herscheid, J.D.M., Tijhuis, M.W., Nivard, R.J.E., De Clercq, E. & Prick, P.A.J.
      Gliotoxin analogues as inhibitors of reverse transcriptase.
      II. Resolution and X-ray crystal structure determination.
      J. Med. Chem., 21: 799-804 (1978).
      


2564. Ottenheijm, H.C.J., Herscheid, J.D.M., Tijhuis, M.W., Ooster­baan, M. & De Clercq, E.
      Gliotoxin analogues as inhibitors of reverse transcriptase. I. Effect of lipophilicity.
      J. Med. Chem., 21: 796-799 (1978).
      


2565. De Clercq, E., Billiau, A., Edy, V.G., Kirk, K.L. & Cohen, L.A.
      Antimetabolic activities of 2-fluoro-L-histidine.
      Biochem. Biophys. Res. Commun., 82: 840-846 (1978).
      


2566. Lebleu, B., Hubert, E., Content, J., De Wit, L., Braude, I.A. & De Clercq, E.
      Translation of mouse interferon mRNA in Xenopus laevis oocytes and in rabbit reticulo­cyte lysates.
      Biochem. Biophys. Res. Commun., 82: 665-673 (1978).
      


2567. De Clercq, E., Stollar, B.D. & Thang, M.N.
      Interferon inducing activity of polyinosinic acid.
      J. Gen. Virol., 40: 203-212 (1978).
      


2568. De Clercq, E., Descamps, J., Huang, G.-F. & Torrence, P.F.
      5-Nitro-2'-deoxyuridine (and 5-nitro-2'-deoxyuridine-5'-monophos­phate) : antiviral activity and in vivo inhibition of thymidylate synthetase.
      Mol. Pharmacol., 14: 422-430 (1978).
      


2569. De Clercq, E.
      Increased resistance of trisomic-21 cells to virus replication: role of interferon.
      Virology, 86: 276-280 (1978).
      


2570. De Clercq, E., Descamps, J., De Somer, P. & Holý, A.
      (S)-9-(2,3-Dihydroxypropyl)adenine : an aliphatic nucleoside ana­log with broad spec­trum antiviral activity.
      Science, 200: 563-565 (1978).
      


2571. De Clercq, E., Descamps, J. & Shugar, D.
      5-Propyl-2'-deoxyuridine : a specific anti-herpes agent.
      Antimicrob. Agents Chemother., 13: 545-547 (1978).
      


2572. Descamps, J. & De Clercq, E.
      Broad-spectrum antiviral activity of pyrazofurin (pyrazomycin).
      In "Current Chemotherapy" (Proceedings of the Tenth Interna­tional Congress of Chemo­therapy, Zürich, Switzerland, 18-23 September, 1977), W. Siegenthaler & R. Lüthy (eds.).
      American Society for Microbiology, Washington, D.C., pp. 354-357 (1978).
      


2573. De Clercq, E., Descamps, J., Torrence, P.F., Krajewska, E. & Shugar, D.
      Antiviral activity of novel deoxyuridine derivatives.
      In "Current Chemotherapy" (Proceedings of the Tenth International Congress of Chemo­therapy, Zürich, Switzerland, 18-23 September, 1977), W. Siegenthaler & R. Lüthy (eds.).
      American Society for Microbiology, Washington, D.C., pp. 352-354 (1978).
      


2574. Lerner, A.M., Reed, S.E., De Clercq, E., Werner, G.H. & Eggers, H.J.
      Chemotherapy of viral diseases.
      In "Current Chemotherapy" (Proceedings of the Tenth International Congress of Chemo­the­rapy, Zürich, Switzerland, 18-23 September, 1977), W. Siegenthaler & R. Lüthy (eds.).
      American Society for Microbiology, Washington, D.C., pp. 22-26 (1978).
      


2575. Janik, B., De Clercq, E. & Sommer, R.G.
      Interferon inducing activity of (A)n.(U)n complexes of varying chain length.
      Biochim. Biophys. Acta, 517: 269-273 (1978).
      


2576. Content, J., Lebleu, B. & De Clercq, E.
      Differential effects of various double-stranded RNAs on protein synthesis in rabbit reticu­locyte lysates.
      Biochemistry, 17: 88-94 (1978).
      


2577. Torrence, P.F., Spencer, J.W., Bobst, A.M., Descamps, J. & De Clercq, E.
      5-O-Alkylated derivatives of 5-hydroxy-2'-deoxyuridine as poten­tial antiviral agents. Anti-herpes activity of 5-propy­nyloxy-2'-deoxyuridine.
      J. Med. Chem., 21: 228-231 (1978).
      


2578. Stollar, B.D., De Clercq, E., Drocourt, J.-L. & Thang, M.N.
      Immunochemical measurement of conformational heterogeneity of poly(inosinic acid).
      Eur. J. Biochem., 82: 339-346 (1978).
      


2579. De Clercq, E., Billiau, A., Ottenheijm, H.C.J. & Herscheid, J.D.M.
      Antireverse transcriptase activity of gliotoxin analogs.
      Biochem. Pharmacol., 27: 635-639 (1978).
      



18 publications in the year 1977



2580. De Clercq, E.
      Novel polynucleotide inducers of human interferon.
      Proceedings Symposium on the "Preparation, Standardization and Clinical Use of Inter­feron" of the Yugoslav Academy of Sciences and Arts, Zagreb, Yugoslavia, June 8-9, 1977, pp. 65-81 (1977).
      


2581. De Clercq, E.
      Interferon induction by polynucleotides : structure-function re­lationship.
      Texas Reports on Biology and Medicine, 35: 29-38 (1977).
      


2582. Torrence, P.F. & De Clercq, E.
      Inducers and induction of interferon.
      Pharmacology and Therapeutics, Part A, Vol. 2: 1-88 (1977).
      


2583. De Clercq, E. & Torrence, P.F.
      Comparative study of various double-stranded RNAs as inducers of human interferon.
      J. Gen. Virol., 37: 619-623 (1977).
      


2584. Dudycz, L., Shugar, D., De Clercq, E. & Descamps, J.
      Synthesis and determination of antiviral activity of 2'(3')-O-methyl derivatives of ribavirin [1-ß-D-ribofuranosyl-1,2,4-tria­zole-3-carboxamide].
      J. Med. Chem., 20: 1354-1356 (1977).
      


2585. De Clercq, E., Huang, G.-F., Torrence, P.F., Fukui, T., Ka­kiuchi, N. & Ikehara, M.
      Biologic activities of poly(2-azaadenylic acid) and poly(2-aza­inosinic acid).
      Nucleic Acids Research, 4: 3643-3653 (1977).
      


2586. Krajewska, E., De Clercq, E. & Shugar, D.
      Virus-induced nucleoside kinase activities in primary rabbit kidney cells.
      Proceedings of the International Conference on Translation of Synthetic and Natural Polynucleotides, Blazejewko near Poznan, Poland, May 10-12, 1977.
      In "Translation of Natural and Synthetic Polynucleotides", ed. A.B. Legocki, University of Agriculture (Poznan), pp. 105-107 (1977).
      


2587. De Clercq, E., Krajewska, E., Descamps, J. & Torrence, P.F.
      Anti-herpes activity of deoxythymidine analogs : specific depen­dence on virus-induced deoxythymidine-deoxycytidine kinase ac­tivity.
      Mol. Pharmacol., 13: 980-984 (1977).
      


2588. De Clercq, E., Janik, B. & Sommer, R.G.
      Effects of ionenes on interferon induction by (I)n.(C)n.
      Antimicrob. Agents Chemother., 11: 756-759 (1977).
      


2589. Torrence, P.F., Bhooshan, B., Descamps, J. & De Clercq, E.
      Improved synthesis and in vitro antiviral activities of 5-cyanouridine and 5-cyano-2'-deoxyuridine.
      J. Med. Chem., 20: 974-976 (1977).
      


2590. De Clercq, E.
      Structuur en vermenigvuldiging van virussen.
      In : "Aanwinsten in de Inwendige Geneeskunde", ed. J. Vanden­broucke.
      European Press, Gent, Vol. 4, pp. 93-115 (1977).
      


2591. De Clercq, E.
      Effect of mouse interferon and polyriboinosinic acid.polyribo-cytidylic acid on L cell tumor growth in nude mice.
      Cancer Res., 37: 1502-1506 (1977).
      


2592. Thang, M.N., Bachner, L., De Clercq, E. & Stollar, B.D.
      A continuous high-molecular weight base-paired structure is not an absolute requirement for a potential polynucleotide inducer of interferon.
      FEBS Letters, 76: 159-165 (1977).
      


2593. De Clercq, E.
      Polynucleotides as inducers of interferon.
      Proceedings of the First Cleveland Symposium on Macromolecules.
      "Structure and Properties of Biopolymers", ed. A.G. Walton.
      Elsevier Scientific Publishing Company, Amsterdam, pp. 217-243 (1977).
      


2594. Torrence, P.F. & De Clercq, E.
      Polyadenylic.polyxanthylic.polyuridylic acid triple helix.
      Biochemistry, 16: 1039-1043 (1977).
      


2595. De Clercq, E., Descamps, J., Krajewska, E. & Shugar, D.
      Antiviral activity of O'-methylated derivatives of adenine ara­binoside.
      Biochem. Pharmacol., 26: 794-797 (1977).
      


2596. Szmigielski, S., Luczak, M., Janiak, M., Kobus, M., Laskowska, B., De Clercq, E. & De Somer, P.
      In vitro and in vivo inhibition of virus multiplication by mi­crowave hyperthermia.
      Arch. Virol., 53: 71-77 (1977).
      


2597. Torrence, P.F., De Clercq, E. & Witkop, B.
      The interaction of polyxanthylic acid with polyadenylic acid.
      Biochim. Biophys. Acta, 475: 1-6 (1977).
      



11 publications in the year 1976



2598. De Clercq, E. & Luczak, M.
      Antiviral activity of carbopol, a cross-linked polycarboxylate.
      Arch. Virol., 52: 151-158 (1976).
      


2599. De Clercq, E., Edy, V.G., Torrence, P.F., Waters, J.A. & Witkop, B.
      Antiviral activity of poly(7-deazainosinic acid)-derived com­plexes in vitro and in vivo.
      Mol. Pharmacol., 12: 1045-1051 (1976).
      


2600. Edy, V.G., Braude, I.A., De Clercq, E., Billiau, A. & De Somer, P.
      Purification of interferon by adsorption chromatography on con­trolled pore glass.
      J. Gen. Virol., 33: 517-521 (1976).
      


2601. De Clercq, E., Edy, V.G. & Cassiman, J.J.
      Chromosome 21 does not code for an interferon receptor.
      Nature, 264: 249-251 (1976).
      


2602. De Clercq, E.
      Genen transfer en ... therapie.
      Tijdschr. Geneesk., 18: 1063-1073 (1976).
      


2603. De Clercq, E., Janik, B. & Sommer, R.G.
      Biological, biochemical and physicochemical evidence for the existence of the poly­adenylate.polyuridylate.poly 2'-fluoro-2'-deoxyuridylate triple-stranded complex.
      Chem.-Biol. Interactions, 14: 113-125 (1976).
      


2604. De Clercq, E. & Luczak, M.
      Intranasal challenge of mice with herpes simplex virus : expe­rimental model for evaluating the efficacy of antiviral drugs.
      J. Infect. Dis., 133 (supplement) : A226-A236 (1976).
      


2605. De Clercq, E., Torrence, P.F., Fukui, T. & Ikehara, M.
      Role of purine N-3 in the biologic activities of poly(A) and poly(I).
      Nucleic Acids Research, 3: 1591-1601 (1976).
      


2606. De Clercq, E., Luczak, M., Shugar, D., Torrence, P.F., Waters, J.A. & Witkop, B.
      Effect of cytosine arabinoside, iododeoxyuridine, ethyldeoxyuri­dine, thiocyanatode­oxyuridine and ribavirin on tail lesion forma­tion in mice infected with vaccinia virus.
      Proc. Soc. Exp. Biol. Med., 151: 487-490 (1976).
      


2607. Torrence, P.F., De Clercq, E. & Witkop, B.
      Triple-helical polynucleotides. Mixed triplexes of the poly(U).poly(A).poly(U) class.
      Biochemistry, 15: 724-734 (1976).
      


2608. De Clercq, E., Torrence, P.F. & Witkop, B.
      Polynucleotide displacement reactions. Detection by interferon induction.
      Biochemistry, 15: 717-724 (1976).
      



22 publications in the year 1975



2609. De Clercq, E.
      Encephalitis induced upon intranasal challenge of mice with her­pes simplex virus : experimental model to assess the clini­cal ef­ficacy of interferon administered exoge­nously.
      Proceedings Symposium on "Clinical Use of Interferon" of the Yu­goslav Academy of Sciences and Arts, Zagreb, Yugoslavia, Oc­tober 1-2, 1977. pp. 129-139 (1975).
      


2610. De Clercq, E., Billiau, A., Hattori, M. & Ikehara, M.
      Inhibition of oncornavirus functions by poly(2-methyl­thioinosinic acid).
      Nucleic Acids Research, 2: 2305-2313 (1975).
      


2611. De Clercq, E., Billiau, A., Torrence, P.F., Waters, J.A. & Witkop, B.
      Antiviral and antimetabolic activities of poly(7-deazaadenylic acid) and poly(7-deazainosinic acid).
      Biochem. Pharmacol., 24: 2233-2238 (1975).
      


2612. De Clercq, E., Torrence, P.F., Waters, J.A. & Witkop, B.
      Antiviral activity of 5-thiocyanatopyrimidine nucleosides.
      Biochem. Pharmacol., 24: 2171-2175 (1975).
      


2613. De Clercq, E., Torrence, P.F., Hobbs, J., Janik, B., De Somer, P. & Witkop, B.
      Anti-complement activity of polynucleotides.
      Biochem. Biophys. Res. Commun., 67: 255-263 (1975).
      


2614. Giziewicz, J., De Clercq, E., Luczak, M. & Shugar, D.
      Antiviral and antimetabolic activities of formycin and its N1-, N2-, 2'-O- and 3'-O-methy­lated derivatives.
      Biochem. Pharmacol., 24: 1813-1817 (1975).
      


2615. De Clercq, E., Stewart II, W.E. & De Somer, P.
      In vitro assay for determination of toxicity to antiviral ac­tivity ratios of double-stranded RNAs.
      Proceedings of the First Intersectional Congress of the Inter­national Association of Microbiological Societies, Tokyo, Japan, September 1-7, 1974. Ed.: T. Hasegawa. Science Council of Japan, Vol. 4, pp. 57-61 (1975).
      


2616. De Clercq, E., Luczak, M., Reepmeyer, J.C., Kirk, K.L. & Cohen, L.A.
      Fluoroimidazoles as antiviral agents and inhibitors of polynu­cleotide biosynthesis.
      Life Sci., 17: 187-194 (1975).
      


2617. De Clercq, E., Edy, V.G. & Cassiman, J.J.
      Non-antiviral activities of interferon are not controlled by chromosome 21.
      Nature, 256: 132-134 (1975).
      


2618. Billiau, A., Edy, V.G., De Clercq, E., Heremans, H. & De Somer, P.
      Influence of interferon on the synthesis of virus particles in oncornavirus carrier cell lines. III. Survey of effects on A-, B- and C-type oncornaviruses.
      Int. J. Cancer, 15: 947-953 (1975).
      


2619. Bachner, L., De Clercq, E. & Thang, M.N.
      Sepharose-bound poly(I).poly(C) : interaction with cells and in­terferon production.
      Biochem. Biophys. Res. Commun., 63: 476-483 (1975).
      


2620. De Clercq, E. & Shugar, D.
      Antiviral activity of 5-ethyl pyrimidine deoxynucleosides.
      Biochem. Pharmacol., 24: 1073-1078 (1975).
      


2621. De Clercq, E. & De Somer, P.
      Are cytotoxicity and interferon-inducing activity of poly(I).poly(C) invariably linked in interferon-treated L cells ?
      J. Gen. Virol., 27: 35-44 (1975).
      


2622. De Clercq, E., Torrence, P.F., De Somer, P. & Witkop, B.
      Biological, biochemical and physicochemical evidence for the existence of the poly­adenylic.polyuridylic.polyinosinic acid triplex.
      J. Biol. Chem. 250: 2521-2531 (1975).
      


2623. Torrence, P.F., De Clercq, E., Waters, J.A. & Witkop, B.
      Failure of duplexes based on polylaurusin [poly(L), "polyformycin B"] to induce inter­feron.
      Biochem. Biophys. Res. Commun., 62: 658-664 (1975).
      


2624. De Clercq, E., Edy, V.G., De Vlieger, H., Eeckels, R. & Desmyter, J.
      Intrathecal administration of interferon in neonatal herpes.
      J. Pediatrics, 86: 736-739 (1975).
      


2625. De Clercq, E.
      Tumor induction by Moloney murine sarcoma virus in athymic nude mice.
      J. Nat. Cancer Inst., 54: 473-477 (1975).
      


2626. De Clercq, E., Darzynkiewicz, E. & Shugar, D.
      Antiviral activity of O'-alkylated derivatives of cytosine ara­binoside.
      Biochem. Pharmacol., 24: 523-527 (1975).
      


2627. De Clercq, E., Torrence, P.F., Witkop, B. & De Somer, P.
      Interferon induction by synthetic polynucleotides : competition between inactive and active polymers.
      "Effects of Interferon on Cells, Viruses and the Immune Sys­tem", Proceedings of a Meeting held at the Gulbenkian Institute of Science, Oeiras, Portugal, September 19-21, 1973. Ed.: A. Geraldes.
      Academic Press, New York and London, pp. 215-236 (1975).
      


2628. De Clercq, E., Hattori, M. & Ikehara, M.
      Antiviral activity of polynucleotides : copolymers of inosinic acid and N2-dimethyl­guanylic acid or 2-methylthioinosinic acid.
      Nucleic Acids Research, 2: 121-129 (1975).
      


2629. De Clercq, E.
      Virale oorsprong van kanker : status praesens.
      Tijdschr. Geneesk., 31: 46-59 (1975).
      


2630. De Clercq, E., Billiau, A., Hobbs, J., Torrence, P.F. & Witkop, B.
      Inhibition of oncornavirus functions by 2'-azido polynu­cleotides.
      Proc. Nat. Acad. Sci. USA, 72: 284-288 (1975).
      



16 publications in the year 1974



2631. De Clercq, E. & Shugar, D.
      Antiviral activity of 5-ethyl pyrimidine nucleosides.
      Proceedings of the VI International Congress of Infectious and Parasitic Diseases, Warsaw, Poland, September 23-27, 1974.
      Preprints Vol. III "Chemotherapy of Viral Diseases, pp. 16-18 (1974).
      


2632. Carter, W.A. & De Clercq, E.
      Viral infection and host defense (Many aspects of viral infec­tion and recovery can be explained by the modulatory role of double-stranded RNA).
      Science, 186: 1172-1178 (1974).
      


2633. De Clercq, E., Torrence, P.F., Witkop, B., Stewart II, W.E. & De Somer, P.
      Interferon induction : tool for establishing interactions among homopolyribonucleotides.
      Science, 186: 835-837 (1974).
      


2634. Torrence, P.F., De Clercq, E., Waters, J.A. & Witkop, B.
      A potent interferon inducer derived from poly(7-deazainosinic acid).
      Biochemistry, 13: 4400-4408 (1974).
      


2635. Stewart II, W.E., De Somer, P. & De Clercq, E.
      Renaturation of inactivated interferons by "defensive re­versible denaturation".
      Prepar. Biochem., 4: 383-393 (1974).
      


2636. Stewart II, W.E., De Somer, P. & De Clercq, E.
      Renaturation of inactivated interferons : requirement for re­duction of a major compo­nent; lack of requirement for reduc­tion of a minor component.
      J. Gen. Virol., 24: 567-570 (1974).
      


2637. Stewart II, W.E., De Somer, P. & De Clercq, E.
      Protective effects of anionic detergents on interferons : re­versible denaturation.
      Biochim. Biophys. Acta, 359: 364-368 (1974).
      


2638. Stewart II, W.E., De Clercq, E. & De Somer, P.
      Stabilisation of interferons by defensive reversible denatura­tion.
      Nature, 249: 460-461 (1974).
      


2639. De Clercq, E. & Stewart II, W.E.
      Integrity of cell-bound poly(I).poly(C).
      J. Gen. Virol., 24: 201-209 (1974).
      


2640. De Clercq, E., Rottman, F.M. & Shugar, D.
      Antiviral activity of polynucleotides : poly 2'-O-ethyladenylic acid and poly 2'-O-ethyluridylic acid.
      FEBS Letters, 42: 331-334 (1974).
      


2641. De Clercq, E.
      Chemotherapie van virale infecties.
      Medikon, 3: 26-32 (1974).
      


2642. Stewart II, W.E. & De Clercq, E.
      Relationship of cytotoxicity and interferon-inducing activity of poly I.poly C to the molecular weights of the homopolymers.
      J. Gen. Virol., 23: 83-89 (1974).
      


2643. De Clercq, E. & Stewart II, W.E.
      Regression of autochthonous Moloney sarcoma virus-induced tu­mors in mice treated with polyriboinosinic acid.polyribocytidylic acid.
      J. Nat. Cancer Inst., 52: 591-594 (1974).
      


2644. De Clercq, E. & De Somer, P.
      Interferon production in rabbit kidney cell cultures exposed to poly(I).poly(C) adsorbed to rabbit red blood cells.
      J. Gen. Virol., 22: 271-275 (1974).
      


2645. De Clercq, E., Torrence, P.F. & Witkop, B.
      Interferon induction by synthetic polynucleotides: importance of purine N-7 and strand­wise rearrangement.
      Proc. Nat. Acad. Sci. USA, 71: 182-186 (1974).
      


2646. De Clercq, E.
      Synthetic interferon inducers.
      Fortschritte der chemischen Forschung, Topics in Current Che­mistry, Ed. F. Boschke.
      Springer-Verlag, Berlin, Heidelberg, New York, 52: 173-208 (1974).
      



16 publications in the year 1973



2647. Stewart II, W.E., De Clercq, E., De Somer, P., Berg, K.,Ogburn, C.A. & Paucker, K.
      Antiviral and non-antiviral activity of highly purified inter­feron.
      Nature, New Biol., 246: 141-143 (1973).
      


2648. De Clercq, E. & Claes, P.J.
      A more sensitive assay system for the detection of RNA-depen­dent DNA polymerase in oncogenic RNA viruses.
      Biochim. Biophys. Acta, 331: 328-332 (1973).
      


2649. De Clercq, E. & De Somer, P.
      Protection of rabbits against local vaccinia virus infection by Brucella abortus and poly­acrylic acid in the absence of sys­temic interferon production.
      Infect. Immun., 8: 669-673 (1973).
      


2650. De Clercq, E., Stewart II, W.E. & De Somer, P.
      Studies on the mechanism of the priming effect of interferon on interferon production by cell cultures exposed to poly(rI).poly(rC).
      Infect. Immun., 8: 309-316 (1973).
      


2651. De Clercq, E. & Janik, B.
      Antiviral activity of polynucleotides : poly 2'-fluoro-2'-de­oxyuridylic acid.
      Biochim. Biophys. Acta, 324: 50-56 (1973).
      


2652. De Clercq, E.
      Antitumor activity of silica gel PF-254 eluate.
      Cancer Res., 33: 2173-2180 (1973).
      


2653. De Clercq, E., Stewart II, W.E. & De Somer, P.
      Poly(rI) more important than poly(rC) in the interferon induc­tion process by poly(rI).poly(rC).
      Virology, 54: 278-282 (1973).
      


2654. Stewart II, W.E. & De Clercq, E.
      Non-antiviral effects of interferon.
      Medikon, 2: 279-284 (1973).
      


2655. De Clercq, E. & Stewart II, W.E.
      Het natuurlijke verloop van een akute virus infektie.
      Tijdschr. Geneesk., 10: 452-461 (1973).
      


2656. De Clercq, E.
      Non-polynucleotide inducers of interferon.
      "Selective Inhibitors of Viral Functions", Ed. W.A. Carter.
      The Chemical Rubber Company Press, Cleveland, Ohio, pp. 177-198 (1973).
      


2657. De Clercq, E. & Stewart II, W.E.
      The breadth of interferon action.
      "Selective Inhibitors of Viral Functions", Ed. W.A. Carter.
      The Chemical Rubber Company Press, Cleveland, Ohio, pp. 81-106 (1973).
      


2658. Black, D.R., Eckstein, F., De Clercq, E. & Merigan, T.C.
      Studies on the toxicity and antiviral activity of various polynu­cleotides.
      Antimicrob. Agents Chemother., 3: 198-206 (1973).
      


2659. De Clercq, E. & De Somer, P.
      Relationship between cell-interaction and antiviral activity of polyriboinosinic acid-polyribocytidylic acid in different cell cultures.
      J. Gen. Virol., 19: 113-123 (1973).
      


2660. De Clercq, E., Stewart II, W.E. & De Somer, P.
      Increased toxicity of double-stranded ribonucleic acid in virus-infected animals.
      Infect. Immun., 7: 167-172 (1973).
      


2661. Stewart II, W.E., De Clercq, E. & De Somer, P.
      Specificity of interferon-induced enhancement of toxicity for double-stranded ribonucleic acids.
      J. Gen. Virol., 18: 237-246 (1973).
      


2662. De Clercq, E.
      Laboratorium diagnosis van virus aandoeningen.
      Medikon, 2: 22-27 (1973).
      



15 publications in the year 1972



2663. Stewart II, W.E., De Clercq, E. & De Somer, P.
      Cellular alteration by interferon : a virus-free system for as­saying interferon.
      J. Virol., 10: 896-901 (1972).
      


2664. De Clercq, E. & De Somer, P.
      Effect of chlorite-oxidized oxyamylose on Moloney sarcoma virus-induced tumor forma­tion in mice.
      Eur. J. Cancer, 8: 535-540 (1972).
      


2665. Stewart II, W.E., De Clercq, E. & De Somer, P.
      Recovery of cell-bound interferon.
      J. Virol., 10: 707-712 (1972).
      


2666. De Clercq, E. & De Somer, P.
      Production of interferon in rabbit cell cultures by mouse L cell-bound poly(rI).poly(rC).
      J. Gen. Virol., 16: 435-439 (1972).
      


2667. De Clercq, E. & Stewart II, W.E.
      Utilization of poly(rI).poly(rC) for controlling virus diseases and tumors still in abey­ance.
      Medikon, 1: 331-337 (1972).
      


2668. De Clercq, E.
      Hyporeactivity to interferon production by double-stranded RNA associated with hypore­activity to antiviral protection and hy­poreactivity to toxicity.
      Proc. Soc. Exp. Biol. Med., 141: 340-345 (1972).
      


2669. De Clercq, E., Zmudzka, B. & Shugar, D.
      Antiviral activity of polynucleotides : role of the 2'-hydroxyl and a pyrimidine 5-methyl.
      FEBS Letters, 24: 137-140 (1972).
      


2670. De Clercq, E., Stewart II, W.E. & De Somer, P.
      Interferon production linked to toxicity of polyriboinosinic acid-polyribocytidylic acid.
      Infect. Immun., 6: 344-347 (1972).
      


2671. Stewart II, W.E., De Clercq, E., Billiau, A., Desmyter, J. & De Somer, P.
      Increased susceptibility of cells treated with interferon to the toxicity of polyriboinosinic.polyribocytidylic acid.
      Proc. Nat. Acad. Sci. USA, 69: 1851-1854 (1972).
      


2672. De Clercq, E. & De Somer, P.
      Mechanism of the antiviral activity resulting from sequential ad­ministration of comple­mentary homopolyribonucleotides to cell cultures.
      J. Virol., 9: 721-731 (1972).
      


2673. De Clercq, E.
      Nucleic acids as interferon inducers.
      Symposium on Virus-Cell Interactions and Viral Antimetabolites of the 7th FEBS Meeting, Varna, Bulgaria, September 20-25, 1971.
      Ed. D. Shugar. Academic Press, London and New York, pp. 65-86 (1972).
      


2674. Chester, T.J., De Clercq, E., Nuwer, M.R. & Merigan, T.C.
      In vivo release of previously cleared interferon by cyclohe­ximide.
      Infect. Immun., 5: 383-388 (1972).
      


2675. De Clercq, E.
      Carcinogenesis by RNA tumor viruses.
      Medikon, 1: 109-127 (1972).
      


2676. De Clercq, E.
      Toekomstmogelijkheden van interferon en interferoninductoren in de menselijke geneeskunde.
      Tijdschr. Geneesk., 4: 307-318 (1972).
      


2677. De Clercq, E., Wells, R.D. & Merigan, T.C.
      Studies on the antiviral activity and cell-interaction of syn­thetic double-stranded polyribo- and polydeoxyribonucleotides.
      Virology, 47: 405-415 (1972).
      



13 publications in the year 1971



2678. De Clercq, E. & De Somer, P.
      Role of interferon in the protective effect of the double-stranded polyribonucleotide against murine tumors induced by Moloney sarcoma virus.
      J. Nat. Cancer Inst., 47: 1345-1355 (1971).
      


2679. De Clercq, E.
      Mechanism of the antiviral activity of synthetic polyanions.
      Thesis (submitted in partial fulfillment of the requirements for the degree of "Geaggregeerde voor het Hoger Onderwijs in de Geneeskunde"), Leuven, (1971).
      


2680. De Clercq, E.
      RNA dependent DNA polymerase.
      Tijdschr. Geneesk., 19: 942-951 (1971).
      


2681. Merigan, T.C. & De Clercq, E.
      Chemically defined non-antiviral interferon inducers : struc­tural requirements and mechanisms.
      Symposium on "Drugs and Cell Regulation", Roswell Park Memorial Institute, Buffalo, New York, September 23-25, 1970, Ed. E. Mi­hich.
      Academic Press, New York and London, pp. 295-303 (1971).
      


2682. Merigan, T.C., De Clercq, E., Eckstein, F. & Wells, R.D.
      Molecular requirements for synthetic RNA to act in interferon stimulation.
      Miles Symposium on "Biological Effects of Polynucleotides", New York, N.Y., June 3-5, 1970, Eds. R.F. Beers & W. Braun. Springer-Verlag, New York, pp. 67-78 (1971).
      


2683. De Clercq, E. & De Somer, P.
      Comparative study of the efficacy of different forms of inter­feron therapy in the treat­ment of mice challenged intranasally with vesicular stomatitis virus (VSV).
      Proc. Soc. Exp. Biol. Med., 138: 301-307 (1971).
      


2684. Nuwer, M.R., De Clercq, E. & Merigan, T.C.
      Interferon clearance rate decreased after repeated injections.
      J. Gen. Virol., 12: 191-194 (1971).
      


2685. De Clercq, E. & De Somer, P.
      Antiviral activity of polyribocytidylic acid in cells primed with polyriboinosinic acid.
      Science, 173: 260-262 (1971).
      


2686. De Clercq, E. & Merigan, T.C.
      Moloney sarcoma virus-induced tumors in mice : inhibition or stimulation by (poly rI).(poly rC).
      Proc. Soc. Exp. Biol. Med., 137: 590-594 (1971).
      


2687. Chester, T.J., De Clercq, E. & Merigan, T.C.
      Effect of separate and combined injections of poly rI.poly rC and endotoxin on reticu­loendothelial activity, interferon and anti­body production in the mouse.
      Infect. Immun., 3: 516-520 (1971).
      


2688. De Clercq, E., Wells, R.D., Grant, R.C. & Merigan, T.C.
      Thermal activation of the antiviral activity of synthetic dou­ble-stranded polyribonucleo­tides.
      J. Mol. Biol., 56: 83-100 (1971).
      


2689. De Clercq, E. & Merigan, T.C.
      Thermal activation of the antiviral activity of synthetic polyri­bonucleotides : influence of DEAE-dextran in various cell cul­tures.
      J. Gen. Virol., 10: 125-130 (1971).
      


2690. De Clercq, E. & Merigan, T.C.
      Bis-DEAE-fluorenone : mechanism of antiviral protection and in­terferon production in the mouse.
      J. Infect. Dis., 123: 190-199 (1971).
      



19 publications in the year 1970



2691. De Clercq, E. & Merigan, T.C.
      Stimulation or inhibition of interferon production depending on time of cycloheximide administration.
      Virology, 42: 799-802 (1970).
      


2692. Merigan, T.C. & De Clercq, E.
      A useful in vitro interferon inducer assay.
      International Symposium on Standardization of Interferon and In­terferon Inducers, Lon­don 1969.
      Symp. Series Immunobiol. Standard., 14: 189-194 (1970).
      


2693. Merigan, T.C., De Clercq, E. & Bausek, G.
      Non-viral inducers of interferon and interference with non-viruses.
      Colloques de l'Institut National de la Santé et de Recherche Médicale, L'Interféron, no. 6: 343-352 (1970).
      


2694. Schonne, E., Billiau, A., De Clercq, E. & De Somer, P.
      Aggregation and molecular weight of rabbit interferon (NDV-RK13).
      Colloques de l'Institut National de la Santé et de la Recherche Médicale, L'Interféron, no. 6: 195-200 (1970).
      


2695. Vandeputte, M., De Clercq, E., Billiau, A., Claesen, M. & De Somer, P.
      The effect of polyacrylic acid on polyoma virus.
      US-Japan Cooperative Seminar on Interferon, Eds. Y. Nagano & H.B. Levy, Igaku Shoin Ltd., Tokyo, pp. 206-212 (1970).
      


2696. Merigan, T.C., De Clercq, E. & Bausek, G.H.
      In vitro studies with polyanionic interferon inducers.
      US-Japan Cooperative Seminar on Interferon, Eds. Y. Nagano & H.B. Levy, Igaku Shoin Ltd., Tokyo, pp. 127-137 (1970).
      


2697. De Clercq, E., Eckstein, F., Sternbach, H. & Merigan, T.C.
      The antiviral activity of thiophosphate-substituted polyribonu­cleotides in vitro and in vivo.
      Virology, 42: 421-428 (1970).
      


2698. De Clercq, E., Nuwer, M.R. & Merigan, T.C.
      The role of interferon in the protective effect of a synthetic double-stranded polyribonu­cleotide against intranasal vesicular stomatitis virus challenge in mice.
      J. Clin. Invest., 49: 1565-1577 (1970).
      


2699. Merigan, T.C., De Clercq, E., Finkelstein, M.S., Clever, L., Walker, S. & Waddell, D.J.
      Clinical studies employing interferon inducers in man and ani­mals.
      Ann. N.Y. Acad. Sci., 173: 746-759 (1970).
      


2700. De Clercq, E., Eckstein, F. & Merigan, T.C.
      Structural requirements for synthetic polyanions to act as in­terferon inducers.
      Ann. N.Y. Acad. Sci., 173: 444-461 (1970).
      


2701. De Somer, P., De Clercq, E., Cocito, C. & Billiau, A.
      The interferon inducer from Brucella.
      Ann. N.Y. Acad. Sci., 173: 274-281 (1970).
      


2702. De Clercq, E., Nuwer, M.R. & Merigan, T.C.
      Potentiating effect of Freund's adjuvant on interferon produc­tion by endotoxin or poly rI.poly rC.
      Infect. Immun., 2: 69-76 (1970).
      


2703. Merigan, T.C., De Clercq, E. & Bausek, G.H.
      Nonviral interferon inducers.
      J. Gen. Physiol., 56: 57-75 (1970).
      


2704. De Clercq, E. & Merigan, T.C.
      Induction of interferon by nonviral agents.
      Arch. Internal Med., 126: 94-108 (1970).
      


2705. De Clercq, E.
      (Poly rI).(poly rC) en double-stranded RNA's : toekomst in de an­tivirale and antitu­morale chemotherapie.
      Tijdschr. Geneesk., 11: 544-559 (1970).
      


2706. De Clercq, E., Eckstein, F., Sternbach, H. & Merigan, T.C.
      Interferon induction by and ribonuclease sensitivity of thio­phosphate substituted polyri­bonucleotides.
      Antimicrob. Agents Chemother.-1969, pp. 187-191 (1970).
      


2707. De Clercq, E. & Merigan, T.C.
      Current concepts of interferon and interferon induction.
      Annu. Rev. Med., 21: 17-46 (1970).
      


2708. De Clercq, E., Wells, R.D. & Merigan, T.C.
      Increase in antiviral activity of polynucleotides by thermal ac­tivation.
      Nature, 226: 364-366 (1970).
      


2709. Claes, P., Billiau, A., De Clercq, E., Desmyter, J., Schonne, E., Vanderhaeghe, H. & De Somer, P.
      Polyacetal carboxylic acids : a new group of antiviral poly­anions.
      J. Virol., 5: 313-320 (1970).
      



8 publications in the year 1969



2710. De Clercq, E. & De Somer, P.
      Prolonged antiviral protection by interferon inducers.
      Proc. Soc. Exp. Biol. Med., 132: 699-703 (1969).
      


2711. De Clercq, E. & Merigan, T.C.
      An active interferon inducer obtained from Hemophilus influen­zae type b.
      J. Immunol., 103: 899-906 (1969).
      


2712. De Clercq, E. & Merigan, T.C.
      Local and systemic protection by synthetic polyanionic inter­feron inducers in mice against intranasal vesicular stomatitis virus.
      J. Gen. Virol., 5: 359-368 (1969).
      


2713. De Clercq, E., Eckstein, F. & Merigan, T.C.
      Interferon induction increased through chemical modification of a synthetic polyribonu­cleotide.
      Science, 165: 1137-1139 (1969).
      


2714. De Clercq, E. & Merigan, T.C.
      Requirement of a stable secondary structure for the antiviral ac­tivity of polynucleotides.
      Nature, 222: 1148-1152 (1969).
      


2715. De Clercq, E.
      Nieuwe perspektieven in de induktie en aktie van interferon.
      Tijdschr. Geneesk., 9: 437-451 (1969).
      


2716. De Clercq, E., De Somer, P. & Schonne, E.
      Concentration of interferon by nucleic acid precipitation.
      Virology, 37: 283-285 (1969).
      


2717. Ormai, S. & De Clercq, E.
      Polymethacrylic acid : effects on lymphocyte output of the tho­racic duct in rats.
      Science, 163: 471-472 (1969).
      



7 publications in the year 1968



2718. De Clercq, E. & De Somer, P.
      Interferon induction by nucleic acid-treated Newcastle disease virus.
      Life Sci., 7: 1319-1325 (1968).
      


2719. De Clercq, E. & De Somer, P.
      Protective effect of interferon and polyacrylic acid in newborn mice infected with a lethal dose of vesicular stomatitis virus.
      Life Sci., 7: 925-933 (1968).
      


2720. De Clercq, E. & De Somer, P.
      Effect of interferon, polyacrylic acid and polymethacrylic acid on tail lesions in mice infected with vaccinia virus.
      Appl. Microbiol., 16: 1314-1319 (1968).
      


2721. De Somer, P., De Clercq, E., Billiau, A., Schonne, E. & Clae­sen, M.
      Antiviral activity of polyacrylic and polymethacrylic acids.
      II. Mode of action in vivo.
      J. Virol., 2: 886-893 (1968).
      


2722. De Somer, P., De Clercq, E., Billiau, A., Schonne, E. & Clae­sen, M.
      Antiviral activity of polyacrylic and polymethacrylic acids.
      I. Mode of action in vitro.
      J. Virol., 2: 878-885 (1968).
      


2723. De Clercq, E.
      Antivirale chemotherapie.
      Tijdschr. Geneesk., 9: 496-505 (1968).
      


2724. De Somer, P., Billiau, A. & De Clercq, E.
      Influence of corticoid administration or stimulation and of N-methylacetamide on inter­feron production in vivo in the rat.
      The Interferons, Ed. G. Rita, Academic Press, pp. 65-81 (1968).
      



4 publications in the year 1967



2725. De Somer, P., De Clercq, E., Billiau, A. & Schonne, E.
      Urinary excretion of interferon in rabbits.
      First Intern. Conf. on Vaccines against Viral and Rickettsial
      Diseases of Man, P.A.H.O., pp. 650-652 (1967).
      


2726. De Somer, P., De Clercq, E. & Billiau, A.
      Influence of whole-body irradiation, cortisol treatment and adrenalectomy on interferon induction in vivo in rats.
      Proc. 2nd Intern. Symp. on Medical and Applied Virology,
      Eds. Sanders & Lennette. Green Publ., pp. 230-243 (1967).
      


2727. De Somer, P., Billiau, A., De Clercq, E. & Schonne, E.
      Rubella virus interference and interferon production.
      Ant. Van Leeuwenhoek, 33: 237-245 (1967).
      


2728. De Somer, P., Billiau, A. & De Clercq, E.
      Inhibition of antibody production in rats and mice by intravenous injection of interferon-inducing amounts of Sindbis virus or E.coli.
      Arch. Ges. Virusforsch., 20: 205-214 (1967).