Synthesis and anti-HIV activity of some novel arylphosphate and H-phosphonate derivatives of 3'-azido-2',3'-dideoxythymidine and 2',3'-didehydro-2',3'-dideoxythymidine.
Phosphate and H-phosphonate derivatives of anti-HIV nucleoside analogues (AZT and d4T) were prepared as potential prodrugs of the bio-active free nucleotide and they were evaluated for their inhibitory effects on the replication of HIV-1 in several cell culture systems. One compound exhibited an important anti-HIV-1 activity and proved to be significantly more efficient than the parent nucleoside.
Cardona
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VM
Laboratoire de Chimie Bio-Organique CNRS ESA 6001, Université de Nice-Sophia Antipolis, Faculté des Sciences, Nice, France.
Ayi
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Aubertin
A M
AM
Guedj
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R
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D010756:Phosphoric Acids / Q000494:pharmacology; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D018119:Stavudine / Q000031:analogs & derivatives*; D015215:Zidovudine / Q000031:analogs & derivatives* / Q000494:pharmacology
D019380:Anti-HIV Agents; D010756:Phosphoric Acids; D018894:Reverse Transcriptase Inhibitors; C068377:2'-azido-2',3'-dideoxythymidine; D015215:Zidovudine; D018119:Stavudine