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

W Hu, Z Guo, X Yi, C Guo, F Chu, G Cheng

Index: Hu, Wenhui; Guo, Zongru; Yi, Xiang; Guo, Changbin; Chu, Fengming; Cheng, Guifang Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 24 p. 5539 - 5544

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Citation Number: 33

Abstract

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.