title: Synthesis, anti-HIV, and cytotoxic activity of new AZT conjugates of steroid acids.
abstract: 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.
authors.affiliation: College of Pharmacy and Pharmaceutical Sciences, Florida A & M University, Tallahassee, Florida 32304, USA.
authors.forename: Zhengqing
authors.initials: Z
authors.lastname: You
authors.forename: A Moshin
authors.initials: AM
authors.lastname: Mian
authors.forename: Ram P
authors.initials: RP
authors.lastname: Agarwal
authors.forename: Henry Joung
authors.initials: HJ
authors.lastname: Lee
mesh_terms: 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
chemical_list: D019380:Anti-HIV Agents; D002793:Cholic Acids; D013256:Steroids; D015215:Zidovudine