Potency of stampidine against multi-nucleoside reverse transcriptase inhibitor resistant human immunodeficiency viruses.
The in vitro potency of stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6) was examined against 8 clinical non-B subtype HIV-1 isolates with resistance to stavudine (STV, d4T), adefovir and tenofovir, 19 clinical zidovudine-resistant HIV-1 isolates, and 6 recombinant HIV-1 clones with multi-resistance against nucleoside reverse transcriptase inhibitors. Stampidine exhibited potent anti-HIV activity against each one of these 33 HIV-1 isolates with subnanomolar to nanomolar IC50 values.
Parker Hughes Institute, Roseville, Minnesota, USA. fatih_uckun@ih.org
Fatih M
FM
Uckun
Taracad K
TK
Venkatachalam
Sanjive
S
Qazi
D019380:Anti-HIV Agents / Q000494:pharmacology*; D054306:Dideoxynucleotides; D024882:Drug Resistance, Viral; D004797:Enzyme-Linked Immunosorbent Assay; D016655:HIV Core Protein p24 / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D008958:Models, Molecular; D009000:Monocytes / Q000187:drug effects / Q000821:virology; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology*; D018119:Stavudine / Q000031:analogs & derivatives* / Q000494:pharmacology; D013938:Thymidine Monophosphate / Q000031:analogs & derivatives* / Q000494:pharmacology
D019380:Anti-HIV Agents; D054306:Dideoxynucleotides; D016655:HIV Core Protein p24; D018894:Reverse Transcriptase Inhibitors; C472384:stampidine; D013938:Thymidine Monophosphate; D018119:Stavudine