Synthesis and biological evaluation of disulfides bearing 1,2,4-triazole moiety as antiproliferative agents

被引：0
作者：
Xue-Feng Wang
Shuai Zhang
Bao-Lin Li
Ji-Jun Zhao
Yu-Ming Liu
Rui-Lian Zhang
Bo Li
Bao-Quan Chen
机构：
[1] Tianjin University of Technology,School of Chemistry and Chemical Engineering, Tianjin Key Laboratory of Organic Solar Cells and Photochemical Conversion
来源：
Medicinal Chemistry Research | 2017年 / 26卷
关键词：
Disulfides; 1,2,4-Triazole; Antiproliferative activity;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of novel nonsymmetrical disulfides bearing 1,2,4-triazole moiety were designed, synthesized, and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 8a–r exhibited good antiproliferative activities, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 8l showed significant antiproliferative activity against SMMC-7721 cells with IC50 value of 2.97 μM. Compound 8f displayed highly effective biological activity against Hela cells with IC50 value of 3.51 μM. Compound 8d exhibited the best inhibitory effect against A549 cells with IC50 value of 2.79 μM. Furthermore, some of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.
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页码：3367 / 3374
页数：7
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