Design, synthesis, and biological evaluation of linear 1-(4-, 3-or 2-methylsulfonylphenyl)-2-phenylacetylenes: a novel class of cyclooxygenase-2 inhibitors

QH Chen, PNP Rao, EE Knaus

Index: Chen, Qiao-Hong; Rao, P. N. Praveen; Knaus, Edward E. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 23 p. 6425 - 6434

Full Text: HTML

Citation Number: 18

Abstract

A group of regioisomeric 1-(methylsulfonylphenyl)-2-phenylacetylenes possessing a COX-2 SO2Me pharmacophore at the para-, meta-or ortho-position of the C-1 phenyl ring, in conjunction with a C-2 phenyl or substituted-phenyl ring substituent (3-F, 3-OMe, 3-OH, 3- OAc, 4-Me), were designed for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors. These target linear 1, 2-diarylacetylenes were synthesized via a palladium-catalyzed ...