Discovering novel quercetin-3-O-amino acid-esters as a new class of Src tyrosine kinase inhibitors

被引：29

作者：

Huang, He ^{[2
]}

Jia, Qi ^{[1
]}

Ma, Jingui ^{[2
]}

Qin, Guangrong ^{[2
]}

Chen, Yingyi ^{[1
]}

Xi, Yonghua ^{[1
]}

Lin, Liping ^{[2
]}

Zhu, Weiliang ^{[2
]}

Ding, Jian ^{[2
]}

Jiang, Hualiang ^{[2
]}

Liu, Hong ^{[2
]}

机构：

[1] Shanghai Univ Tradit Chinese Med, Sch Chinese Med, Shanghai 201203, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 05期

基金：

中国国家自然科学基金;

关键词：

Quercetin; Amino acid; Src; EGFR; Inhibitor; QUERCETIN; GROWTH;

D O I：

10.1016/j.ejmech.2008.09.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quercetin-3-O-amino acid-esters, a new type of quercetin derivatives, were successfully prepared for the first time. Different from quercetin, the novel compounds show higher selectivity as inhibitors against Src tyrosine kinase (IC50 values ranging from 3.2 mu M to 9.9 mu M) than against EGFR tyrosine kinase. Molecular docking reveals that both hydrophobic and hydrogen bonding interactions are important to the selectivity. Therefore, this study provides a new promising scaffold for further development of new anticancer drugs targeting Src tyrosine kinase. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：1982 / 1988

页数：7

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