Synthesis and in vitro antiproliferative evaluation of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety

被引:23
作者
Zhao, Ji-Jun [1 ]
Wang, Xue-Feng [1 ]
Li, Bao-Lin [1 ]
Zhang, Rui-Lian [1 ]
Li, Bo [1 ]
Liu, Yu-Ming [1 ]
Li, Cai-Wen [1 ]
Liu, Jin-Biao [1 ]
Chen, Bao-Quan [1 ]
机构
[1] Tianjin Univ Technol, Dept Chem & Chem Engn, Tianjin 300384, Peoples R China
基金
中国国家自然科学基金;
关键词
Nonsymmetrical disulfides; 1,3,4-Oxadiazole; Antiproliferative activity; BIOLOGICAL EVALUATION; ACETOHYDROXYACID SYNTHASE; ANTITUMOR-ACTIVITY; ANTICANCER AGENTS; DERIVATIVES; INHIBITORS; DESIGN; 3D-QSAR; SERIES;
D O I
10.1016/j.bmcl.2016.08.014
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against SMMC-7721, Hela and A549 human cancer cell lines by CCK-8 assay. The preliminary bioassay results demonstrated that all tested compounds 7a-7o exhibited antiproliferation with different degrees, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 7j showed significant antiproliferative activity against SMMC-7721 cells with IC50 value of 3.40 mu M. Compound 7a displayed highly effective biological activity against Hela cells with IC50 value of 4.26 mu M. Compound 7g exhibited the best inhibitory effect against A549 cells with IC50 value of 6.26 mu M. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4414 / 4416
页数:3
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