Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides.
Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides.
复制标题
DOI：
10.1021/jm00081a015
复制
发表时间：
1992-02
影响因子：
7.3
通讯作者：
J. Secrist;R. M. Riggs;K. Tiwari;J. Montgomery
中科院分区：
文献类型：
--
作者：
J. Secrist;R. M. Riggs;K. Tiwari;J. Montgomery
合成了一系列2‘，3’-二脱氧-4‘-硫代核苷类似物，包括4’-硫代二碘(17)、4‘-硫代C(27)和4’-硫代AZT(34)，并评价了它们对人类免疫缺陷病毒(HIV)的抑制活性。报道了以L-谷氨酸为起始原料，立体定向合成2，3-二脱氧-4-硫代呋喃糖基碳水化合物前体11的方法。2‘，3’-二脱氧-4‘-硫代胞苷(27)具有较强的体外抗人类免疫缺陷病毒活性。
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.