SYNTHESIS AND ANTI-HIV ACTIVITY OF 4'-THIO-2',3'-DIDEOXYNUCLEOSIDES

被引：81
作者：
SECRIST, JA
RIGGS, RM
TIWARI, KN
MONTGOMERY, JA
机构：
[1] Kettering-Meyer Laboratory, Southern Research Institute, Birmingham, Alabama 35255-5305
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 03期
关键词：
D O I：
10.1021/jm00081a015
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2',3'-dideoxy-4'-thionucleoside analogues of purines and pyrimidines, including 4'-thioddI (17), 4'-thioddC (27), and 4'-thioAZT (34), were synthesized and evaluated for their inhibitory activity against human immunodeficiency virus (HIV). A stereospecific synthesis of the 2,3-dideoxy-4-thioribofuranosyl carbohydrate precursor 11 starting with L-glutamic acid is described. 2',3'-Dideoxy-4'-thiocytidine (27) displayed significant, but modest activity in vitro against human immunodeficiency virus.
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页码：533 / 538
页数：6
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