Document 0413
 DOCN  M9650413
 TI    Synthesis and antiviral activity of 2'-deoxy-4'-thio purine nucleosides.
 DT    9605
 AU    Van Draanen NA; Freeman GA; Short SA; Harvey R; Jansen R; Szczech G;
       Koszalka GW; Division of Experimental Therapy, Burroughs Wellcome
       Company,; Research Triangle Park, North Carolina 27709, USA.
 SO    J Med Chem. 1996 Jan 19;39(2):538-42. Unique Identifier : AIDSLINE
       MED/96145189
 AB    A series of 2'-deoxy-4'-thioribo purine nucleosides was prepared by
       trans-N-deoxyribosylase-catalyzed reaction of 2'-deoxy-4'-thiouridine
       with a variety of purine bases. This synthetic procedure is an
       improvement over methods previously used to prepare purine 4'-thio
       nucleosides. The compounds were tested against hepatitis B virus (HBV),
       human cytomegalovirus (HCMV), herpes simplex virus (HSV-1 and HSV-2),
       varicella zoster virus (VZV), and human immunodeficiency virus (HIV-1).
       Cytotoxicity was determined in a number of cell lines. Several compounds
       were extremely potent against HBV and HCMV and had moderate to severe
       cytotoxicity in vitro. The lead compound from the series,
       2-amino-6-(cyclopropylamino)purine 2'-deoxy-4'-thioriboside, was the
       most potent and selective agent against HCMV and HBV replication in
       vitro; however, this analogue was nephrotoxic when tested in vivo.
 DE    Antiviral Agents/CHEMISTRY/*CHEMICAL SYNTHESIS/*PHARMACOLOGY  Cell Line
       Cell Survival/DRUG EFFECTS  Herpesviridae/DRUG EFFECTS  Human
       HIV-1/DRUG EFFECTS  Purine Nucleosides/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).