Synthesis and biological evaluation of substituted 2-sulfonyl-phenyl-3-phenyl-indoles: A new series of selective COX-2 inhibitors

被引：105

作者：

Hu, WH

Guo, ZR ^{[1
]}

Chu, FM

Bai, AP

Yi, X

Cheng, GF

Li, J

机构：

[1] Chinese Acad Med Sci, Dept Synthet Med Chem, Beijing 100050, Peoples R China

[2] Peking Union Med Coll, Beijing 100050, Peoples R China

[3] Chinese Acad Med Sci, Inst Mat Med, Dept Pharmacol, Beijing 100050, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 07期

基金：

中国国家自然科学基金;

关键词：

D O I：

10.1016/S0968-0896(03)00046-4

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 new series of substituted 2-sulfonyphenyl-3-phenyl-indole derivatives were synthesized and evaluated for their ability to inhibit COX-2 and COX-lenzymes. Most of the compounds synthesized were found to be highly potent and selective inhibitors of COX-2. This work led to the discovery of 2-aminosulfonylphenyl-3-phenyl-indole 5a which possesses higher activity and selectivity for COX-2 than Celecoxib both in vitro and in vivo. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1153 / 1160

页数：8

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