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

W Hu, Z Guo, F Chu, A Bai, X Yi, G Cheng…

Index: Hu, Wenhui; Guo, Zongru; Chu, Fengming; Bai, Aiping; Yi, Xiang; Cheng, Guifang; Li, Jing Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 7 p. 1153 - 1160

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Citation Number: 93

Abstract

A new series of substituted 2-sulfonyphenyl-3-phenyl-indole derivatives were synthesized and evaluated for their ability to inhibit COX-2 and COX-1enzymes. 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.