Stampidine is a potent inhibitor of Zidovudine- and nucleoside analog reverse transcriptase inhibitor-resistant primary clinical human immunodeficiency virus type 1 isolates with thymidine analog mutations.
We report the antiretroviral activity of stavudine-5'-(p-bromophenyl methoxyalaninyl phosphate) (stampidine [STAMP]), a novel aryl phosphate derivative of stavudine, against primary clinical human immunodeficiency virus type 1 (HIV-1) isolates. STAMP inhibited each one of nine clinical HIV-1 isolates of non-B envelope subtype and 20 genotypically and phenotypically nucleoside analog reverse transcriptase inhibitor-resistant HIV-1 isolates at subnanomolar to low-nanomolar concentrations.
Uckun
Fatih M
FM
Drug Discovery Program, Departments of Virology, Bioinformatics, Immunology, and Chemistry, Parker Hughes Institute, St. Paul. Parker Hughes Center for Clinical Immunology, Roseville, Minnesota 55113, USA. fatih_uckun@ih.org
Pendergrass
Sharon
S
Venkatachalam
T K
TK
Qazi
Sanjive
S
Richman
Douglas
D
D019380:Anti-HIV Agents / Q000494:pharmacology*; D054306:Dideoxynucleotides; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000821:virology; D054303:HIV Reverse Transcriptase / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D009705:Nucleosides / Q000494:pharmacology*; D010641:Phenotype; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology*; D018119:Stavudine / Q000031:analogs & derivatives / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013936:Thymidine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D013938:Thymidine Monophosphate / Q000031:analogs & derivatives / Q000494:pharmacology*; D015215:Zidovudine / Q000494:pharmacology*
D019380:Anti-HIV Agents; D054306:Dideoxynucleotides; D009705:Nucleosides; D018894:Reverse Transcriptase Inhibitors; C472384:stampidine; D013938:Thymidine Monophosphate; D015215:Zidovudine; D018119:Stavudine; D054303:HIV Reverse Transcriptase; D013936:Thymidine