Synthesis, anti-HIV, and cytotoxic activity of new AZT conjugates of steroid acids.
In an attempt to discover potent anti-HIV agents devoid of the serious toxicity of the current HIV-reverse transcriptase inhibitors, three steroid prodrugs of AZT have been synthesized and their anti-HIV profiles determined with CEM-SS cell line. Two of the prodrugs were active against HIV, though weaker than AZT. The third agent was totally inactive against HIV. However, it demonstrated remarkably high anti-growth activities. Further experiments established that growth inhibition of the third agent was caused by induction of apoptosis rather than general necrosis.
You
Zhengqing
Z
College of Pharmacy and Pharmaceutical Sciences, Florida A & M University, Tallahassee, Florida 32304, USA.
Mian
A Moshin
AM
Agarwal
Ram P
RP
Lee
Henry Joung
HJ
D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D017209:Apoptosis; D002455:Cell Division; D002460:Cell Line; D002793:Cholic Acids / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D006801:Humans; D013256:Steroids / Q000737:chemistry*; D013997:Time Factors; D015215:Zidovudine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
D019380:Anti-HIV Agents; D002793:Cholic Acids; D013256:Steroids; D015215:Zidovudine