Hu Wenhui, Guo Zongru, Yi Xiang, Guo Changbin, Chu Fengming, Cheng Guifang
Department of Synthetic Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, PR China.
Bioorg Med Chem. 2003 Dec 1;11(24):5539-44. doi: 10.1016/j.bmc.2003.09.008.
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.