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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