Synthesis of the novel elemonic acid derivatives as Pin1 inhibitors

被引：8

作者：

Li, Xiaojing ^{[1
]}

Zhou, Qingtong ^{[2
]}

Zhang, Na ^{[1
]}

Zhang, Shuzhi ^{[1
]}

Zhao, Rui ^{[1
]}

Liu, Dan ^{[1
]}

Jing, Yongkui ^{[3
]}

Zhao, Linxiang ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China

[2] Shenyang Pharmaceut Univ, Dept Pharmacol, Shenyang 110016, Peoples R China

[3] Mt Sinai Sch Med, Dept Med, New York, NY 10029 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 24期

基金：

中国国家自然科学基金;

关键词：

Elemonic acid; Tirucallane; Triterpenoid; Pin1; inhibition; Anticancer; PROLYL ISOMERASE PIN1; TRITERPENE ACIDS; OVEREXPRESSION; TARGET; RESIN;

D O I：

10.1016/j.bmcl.2014.10.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of elemonic acid derivatives were synthesized and evaluated for their inhibitory activity on Pin1. Five compounds displayed significantly improved ability to inhibit Pin1 activity at micromolar levels. Compound 10 with 2-carboxylmethylene was the most active one with an IC50 value of 0.57 mu M. The docking models of Pin1 support that introduction of an acidic group to elemonic acid enhance the Pin1 inhibitory activity. (C) 2014 Published by Elsevier Ltd.

引用

页码：5612 / 5615

页数：4

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