Document 2240
 DOCN  M94A2240
 TI    beta-L-2',3'-dideoxy-5-fluorocytidine (L-FDDC) a novel potent and
       selective inhibitor of HIV and HBV replication in vitro.
 DT    9412
 AU    Sommadossi JP; Faraj A; Schinazi R; Gosselin G; Imbach JL; Univ. of AL
       at Birmingham 35294.
 SO    Int Conf AIDS. 1994 Aug 7-12;10(1):35 (abstract no. 112A). Unique
       Identifier : AIDSLINE ICA10/94370335
 AB    beta-L-2',3'-dideoxy-5-fluorocytidine (L-FDDC) potently inhibited HIV-1,
       and HIV-2 replication in vitro in various cell lines. L-FDDC exhibited
       an EC90 of 0.15 microM in peripheral blood mononuclear cells infected by
       HIV-1. L-FDDC showed the highest selectivity index (9000) as compared to
       L-DDC (37), FDDC (35), and AZT (100) when the index was determined
       relative to human bone marrow progenitor cells. Using a
       poly(rI)n.oligo(dC)10-15 as a template primer, the 5'-triphosphate of
       L-FDDC (L-FDDCTP) competitively inhibited HIV-1 RT with a Ki of 1.00
       microM, with respect to dCTP. L-FDDCTP did not inhibit human DNA
       polymerases alpha, beta, and gamma up to 50 microM. L-FDDC was also a
       potent and selective inhibitor of HBV replication with an EC90 of 0.30
       microM when HBV virion levels were measured in transfected 2.2.15 cells.
       The EC90 values for L-DDC and L-FTC were 1.1 and 0.15 microM
       respectively. L-FDCCTP inhibited woodchuck HBV DNA polymerase with an
       IC50 approximating 1.75 microM. These data suggest that further
       development of L-FDDC for treatment of HIV and HBV infections merits
       consideration.
 DE    Antiviral Agents/*PHARMACOLOGY  Binding, Competitive/DRUG EFFECTS  Cell
       Line  Comparative Study  Hepatitis B Virus/*DRUG EFFECTS/PHYSIOLOGY
       Hepatitis Virus, Woodchuck/DRUG EFFECTS  Human  HIV-1/*DRUG
       EFFECTS/PHYSIOLOGY  HIV-2/*DRUG EFFECTS/PHYSIOLOGY  Reverse
       Transcriptase/METABOLISM  Transfection  Virus Replication/*DRUG EFFECTS
       Zalcitabine/*ANALOGS & DERIVATIVES/*PHARMACOLOGY
       Zidovudine/PHARMACOLOGY  MEETING ABSTRACT

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