Discovery of 2-phenyl-3-sulfonylphenyl-indole derivatives as a new class of selective COX-2 inhibitors

被引：61

作者：

Hu, WH

Guo, ZR ^{[1
]}

Yi, X

Guo, CB

Chu, FM

Cheng, GF

机构：

[1] Chinese Acad Med Sci, Inst Mat Med, Dept Synth Med Chem, Beijing 100050, Peoples R China

[2] Peking Union, Coll Med, 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 / 24期

基金：

中国国家自然科学基金;

关键词：

D O I：

10.1016/j.bmc.2003.09.008

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：

2-Sulfonylphenyl-3-phenyl-indole derivatives have been reported to be highly potent and selective COX-2 inhibitors previously. In this paper, the regio-isomeric analogues-2-phenyl-3-sulfonylphenyl-indoles were identified as potent and selective COX-2 inhibitors. This work led to the discovery of compounds 4a and 8a possessing higher activity than Celecoxib on cellular assay. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：5539 / 5544

页数：6

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