ACTIVITIES OF THE 4 OPTICAL ISOMERS OF 2',3'-DIDEOXY-3'-THIACYTIDINE (BCH-189) AGAINST HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 IN HUMAN-LYMPHOCYTES

被引：276
作者：
SCHINAZI, RF
CHU, CK
PECK, A
MCMILLAN, A
MATHIS, R
CANNON, D
JEONG, LS
BEACH, JW
CHOI, WB
YEOLA, S
LIOTTA, DC
机构：
[1] EMORY UNIV,DEPT CHEM,ATLANTA,GA 30322
[2] VET AFFAIRS MED CTR,DECATUR,GA 30033
[3] UNIV GEORGIA,COLL PHARM,DEPT MED CHEM & PHARMACOGNOSY,ATHENS,GA 30602
来源：
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 1992年 / 36卷 / 03期
关键词：
D O I：
10.1128/AAC.36.3.672
中图分类号：
Q93 [微生物学];
学科分类号：
071005 ; 100705 ;
摘要：
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-mu-M. The relative order of potencies for the isomers was beta-L-(-) > beta-DL-(+/-) racemic > beta-D-(+) > alpha-L(+) > alpha-D-(-). The beta-L-(-) enantiomer was as potent as 3'-azido-3'-deoxythymidine.
引用
收藏
页码：672 / 676
页数：5
相关论文
共 32 条
1234