Synthesis and biological activity, evaluation of emodin quaternary ammonium salt derivatives as potential anticancer agents

被引：32

作者：

Wang, Wenfeng ^{[2
]}

Bai, Zedong ^{[1
]}

Zhang, Fengsen ^{[2
]}

Wang, Conghui ^{[2
]}

Yuan, Yaofeng ^{[2
]}

Shao, Jingwei ^{[1
]}

机构：

[1] Fuzhou Univ, Coll Chem & Chem Engn, Dept Pharmaceut Engn, Fuzhou 350108, Fujian, Peoples R China

[2] Fuzhou Univ, Coll Chem & Chem Engn, Inst Organ Chem, Fuzhou 350108, Fujian, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 56卷

基金：

中国博士后科学基金;

关键词：

Emodin derivatives; Anticancer activity; Apoptosis; Quaternary ammonium salt; ALOE-EMODIN; DNA-BINDING; HK-2; CELLS; IN-VITRO; APOPTOSIS; PATHWAY; ACTIVATION; VIVO;

D O I：

10.1016/j.ejmech.2012.07.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Twenty-six emodin derivatives (17 novel) which attach quaternary ammonium salt were synthesized and evaluated for their anticancer activities in vitro and in vivo. Compounds 11g + 12g and 11h + 12h had more significant antiproliferative ability against three cancer cell lines and low cytotoxicity to HELF. 11g + 12g and 11 h + 12h induced AGS cell apoptosis and arrested cell cycle at the G(0)/G(1) phase in a dose-dependent manner. Furthermore, the activities of the caspase-3, -9 enzymes were increased in the treated cells. In vivo studies revealed that compounds 11g + 12g and 11h + 12h showed significant antitumor activity compared with controlled group. (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：320 / 331

页数：12

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