Synthesis and in vitro antitumor activity of new butenolide-containing dithiocarbamates

被引：58
|
作者：
Wang, Xiao-Juan [1 ,2 ]
Xu, Hai-Wei [1 ,3 ]
Guo, Lin-Lin [1 ,3 ]
Zheng, Jia-Xin [1 ,3 ]
Xu, Bo [1 ,3 ]
Guo, Xiao [1 ,3 ]
Zheng, Chen-Xin [1 ,3 ]
Liu, Hong-Min [1 ,2 ,3 ]
机构：
[1] Zhengzhou Univ, New Drug Res & Dev Ctr, Zhengzhou 450001, Peoples R China
[2] Zhengzhou Univ, Dept Chem, Zhengzhou 450052, Peoples R China
[3] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 10期
基金：
中国国家自然科学基金; 中国博士后科学基金;
关键词：
Butenolides; Dithiocarbamate; Anti-tumor activity; DERIVATIVES; CHEMISTRY; CANCER; CYTOTOXICITY; SULFORAMATE; ANALOGS; BINDING; TUMOR; ACID;
D O I：
10.1016/j.bmcl.2011.03.029
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Three series of butenolide-containing dithiocarbamates were designed and synthesized. Their anti-tumor activity in vitro was evaluated. Among them compound I-14 exhibited broad spectrum anti-cancer activity against five human cancer cell lines with IC50 <30 mu M. Structure-activity relationship analysis showed that the introduction of dithiocarbamate side chains on the C-3 position of butenolide was crucial for anti-tumor activity. (C) 2011 Elsevier Ltd. All rights reserved.
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页码：3074 / 3077
页数：4
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