       Document 0871
 DOCN  M9650871
 TI    2-amino-9-(3-azido-2,3-dideoxy-beta-D-erythro-pentofuranosyl)-6-s-
       ubstituted-9H-purines: synthesis and anti-HIV activity.
 DT    9605
 AU    Freeman GA; Shaver SR; Rideout JL; Short SA; Burroughs Wellcome Co.,
       Division of Organic Chemistry, Research; Triangle Park, NC 27709, USA.
 SO    Bioorg Med Chem. 1995 Apr;3(4):447-58. Unique Identifier : AIDSLINE
       MED/96172310
 AB    A series of
       2-amino-9-(3-azido-2,3-dideoxy-beta-D-erythro-pentofuranosyl)-6-
       substituted-9H-purines was synthesized and tested for the ability to
       protect MT4 cells from the cytopathic effect of HIV-1IIIB. These
       compounds were prepared by a combination of chemical and enzymatic
       reactions. Some of the nucleoside analogs with 6-alkoxy, 6-alkylamino,
       or 6-arylamino substituents were active against HIV-1IIIB. Their IC50
       values were in the range of 2-60 microM. In contrast, analogs with
       6-thio, 6-alkylthio, 6-methyl, or 6-carbonitrile substituents did not
       protect cells from the cytopathic effect of HIV infection.
 DE    Antiviral Agents/*CHEMISTRY/CHEMICAL SYNTHESIS/*PHARMACOLOGY  Cell Line,
       Transformed/DRUG EFFECTS  Cytopathogenic Effect, Viral/DRUG EFFECTS
       Dideoxynucleosides/*CHEMISTRY  Guanosine/ANALOGS & DERIVATIVES/CHEMISTRY
       Human  HIV-1/*DRUG EFFECTS  Lactobacillus/ENZYMOLOGY
       Pentosyltransferases/METABOLISM  Purines/CHEMISTRY/METABOLISM
       Structure-Activity Relationship  T-Lymphocytes/CYTOLOGY/VIROLOGY
       Thymidine/CHEMISTRY/METABOLISM  Zidovudine/*ANALOGS &
       DERIVATIVES/CHEMICAL SYNTHESIS/PHARMACOLOGY  JOURNAL ARTICLE

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

