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.

引用

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页码：3074 / 3077

页数：4

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