Activities of the four optical isomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) against human immunodeficiency virus type 1 in human lymphocytes.
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.
Schinazi
R F
RF
Department of Pediatrics, Emory University School of Medicine, Atlanta, Georgia 30322.
Chu
C K
CK
Peck
A
A
McMillan
A
A
Mathis
R
R
Cannon
D
D
Jeong
L S
LS
Beach
J W
JW
Choi
W B
WB
Yeola
S
S
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
D000998:Antiviral Agents; D019259:Lamivudine; D015215:Zidovudine; D016047:Zalcitabine