title: Activities of the four optical isomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) against human immunodeficiency virus type 1 in human lymphocytes.
abstract: Four different isomers of 2',3'-dideoxy-3'-thiacytidine [beta-DL-(+-)-BCH-189] were evaluated in primary human lymphocytes infected with human immunodeficiency virus type 1. The beta-L-(-) isomer was the most potent enantiomer, with a median effective concentration of 1.8 nM and no discernible cytotoxicity up to 100 microM. The relative order of potencies for the isomers was beta-L-(-) greater than beta-DL-(+-) racemic greater than beta-D-(+) greater than alpha-L-(+) greater than alpha-D-(-). The beta-L-(-) enantiomer was as potent as 3'-azido-3'-deoxythymidine.
authors.affiliation: Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322.
authors.forename: R F
authors.initials: RF
authors.lastname: Schinazi
authors.forename: C K
authors.initials: CK
authors.lastname: Chu
authors.forename: A
authors.initials: A
authors.lastname: Peck
authors.forename: A
authors.initials: A
authors.lastname: McMillan
authors.forename: R
authors.initials: R
authors.lastname: Mathis
authors.forename: D
authors.initials: D
authors.lastname: Cannon
authors.forename: L S
authors.initials: LS
authors.lastname: Jeong
authors.forename: J W
authors.initials: JW
authors.lastname: Beach
authors.forename: W B
authors.initials: WB
authors.lastname: Choi
authors.forename: S
authors.initials: S
authors.lastname: Yeola
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D019259:Lamivudine; D008214:Lymphocytes / Q000187:drug effects* / Q000382:microbiology; D008826:Microbial Sensitivity Tests; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D016047:Zalcitabine / Q000031:analogs & derivatives* / Q000494:pharmacology; D015215:Zidovudine / Q000494:pharmacology
chemical_list: D000998:Antiviral Agents; D019259:Lamivudine; D015215:Zidovudine; D016047:Zalcitabine