Design, synthesis and evaluation of novel sulfonyl pyrrolidine derivatives as matrix metalloproteinase inhibitors

被引：26

作者：

Cheng, Xian-Chao ^{[1
]}

Wang, Qiang ^{[1
]}

Fang, Hao ^{[1
]}

Tang, Wei ^{[2
]}

Xu, Wen-Fang ^{[1
]}

机构：

[1] Shandong Univ, Inst Med Chem, Sch Pharmaceut Sci, Jinan 250012, Peoples R China

[2] Univ Tokyo, Hepatobiliary Pancreat Surg Div, Dept Surg, Grad Sch Med, Tokyo 1138655, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 10期

基金：

国家高技术研究发展计划(863计划);

关键词：

sulfonyl pyrrolidine derivatives; synthesis; MMP-2; inhibitors; IC50;

D O I：

10.1016/j.bmc.2008.04.027

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel sulfonyl pyrrolidine derivatives were designed, synthesized and assayed for their inhibitory activities on matrix metalloproteinase 2 (MMP-2) and aminopeptidase N (AP-N). The results showed that these pyrrolidine derivatives exhibited highly selective inhibition against MMP-2 as compared with AP-N. Compounds 6a-d were more potent MMP-2 inhibitors than the positive control LY52. The structure-activity relationships were also briefly discussed. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5398 / 5404

页数：7

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