Abstract
A new class of 1,3-diphenylprop-2-yn-1-ones possessing a p-MeSO 2 COX-2 phamacophore on the C-3 phenyl ring was designed for evaluation as dual inhibitors of cyclooxygenase (COX) and lipoxygenase (LOX). Among the group of compounds evaluated, 1-(4-fluorophenyl)-3-(4-methanesulfonylphenyl)prop-2-yn-1-one ( 11j) exhibited excellent COX-2 inhibitory potency (COX-2 IC 50 = 0.1 μM) and selectivity (SI = 300), whereas 1-(4-cyanophenyl)-3-(4-methanesulfonylphenyl)prop-2-yn-1-one ( 11d) exhibited an optimal combination of COX and LOX inhibition (COX-2 IC 50 = 1.0 μM; COX-2 SI = 31.5; 5-LOX IC 50 = 1.0 μM; 15-LOX IC 50 = 3.2 μM).
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