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).