ChemInform Abstract: Diaryl Indenes and Benzofurans: Novel Classes of Potent and Selective Cyclooxygenase-2 Inhibitors.

Novel series of diaryl indenes and benzofurans have been shown to be potent and selective COX-2 inhibitors. A structure-activity relationship study suggests that the conversion of sulfones to sulfonamides affords potent, but slightly less selective COX-2 inhibitors, and that for benzofurans the 3-halo-4-methoxyphenyl sulfonamide analogs are more selective than the corresponding 4-fluorophenyl analog.