Document 0694
 DOCN  M9650694
 TI    Synthesis and anti-HIV activity of steroidal prodrugs of
       3'-azido-3'-deoxythymidine (AZT).
 DT    9605
 AU    Balagopala MI; Ollapally AP; Lee HJ; Department of Chemistry, Florida A.
       & M. University, Tallahassee; 32307, USA.
 SO    Cell Mol Biol (Noisy-le-grand). 1995;41 Suppl 1:S1-7. Unique Identifier
       : AIDSLINE MED/96171628
 AB    A total of seven steroidal prodrugs of AZT were synthesized and tested
       in vitro for their anti-HIV activity. Three of them were steroidal
       carboxylic esters prepared from steroidal 17 beta-carboxylic acids and
       AZT. The remaining four were alkyl steroidal phospho-triesters of AZT.
       These prodrugs were synthesized using known procedures. Preliminary
       results of in vitro anti-HIV activity screening showed that all of these
       prodrugs were active against HIV. While carboxylic esters showed
       comparable anti-HIV activity to that of AZT, phosphotriesters were less
       active than AZT. The therapeutic indices of all these prodrugs are
       comparable to that of AZT.
 DE    Androstenols/CHEMISTRY/CHEMICAL SYNTHESIS/*PHARMACOLOGY  Antiviral
       Agents/CHEMISTRY/CHEMICAL SYNTHESIS/*PHARMACOLOGY  Biotransformation
       Cell Survival  Comparative Study  CD4-Positive T-Lymphocytes/VIROLOGY
       Drug Screening  Human  HIV-1/*DRUG EFFECTS  Leukemia, Lymphocytic,
       Acute/PATHOLOGY  Molecular Structure  Nuclear Magnetic Resonance
       Prodrugs/CHEMISTRY/CHEMICAL SYNTHESIS/*PHARMACOLOGY  Support, U.S.
       Gov't, P.H.S.  Tumor Cells, Cultured  Zidovudine/*ANALOGS &
       DERIVATIVES/*ADMINISTRATION & DOSAGE/  CHEMISTRY/CHEMICAL
       SYNTHESIS/PHARMACOLOGY  JOURNAL ARTICLE

       SOURCE: National Library of Medicine.  NOTICE: This material may be
       protected by Copyright Law (Title 17, U.S.Code).