Synthesis and antitumor evaluation of some 1,3,4-oxadiazole-2(3H)-thione and 1,2,4-triazole-5(1H)-thione derivatives

被引：0
作者：
ChengTao Feng
LingDong Wang
YuGang Yan
Jian Liu
ShaoHua Li
机构：
[1] Nanchang University Medical College,Department of Pharmacy
[2] Huainan Union University,Department of Chemistry
来源：
Medicinal Chemistry Research | 2012年 / 21卷
关键词：
1,3,4-Oxadiazole-2(3; )-thione; 1,2,4-Triazole-5(1; )-thione; Synthesis; Antitumor activity; Docking study;
D O I：
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中图分类号：
学科分类号：
摘要：
A series of 1,3,4-oxadiazole-2-thione and 1,2,4-triazole-5-thione derivatives have been successfully synthesized and studied for their antitumor activity. These compounds were prepared from carboxylic acids and chiral aminoacid esters. The prepared compounds were evaluated for their cytotoxicity against cancer in vitro using hydroxyurea (HU) as positive control. A fair number of compounds were found to have significant antitumor activity. To study the molecular basis of interaction and affinity of binding of the target molecules, all the compounds were docked into the ATPase domain of TP-II and tubulin using Schrödinger.
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页码：315 / 320
页数：5
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