Sulfonamide derivatives of styrylheterocycles as a potent inhibitor of COX-2-mediated prostaglandin E2 production

The overproduction of prostaglandin E2 (PGE2) plays an important role in a variety of pathophysiological processes including inflammation and carcinogenesis. Therefore, the modulation of PGE2 production is a promising target in the design of chemotherapeutic agents. In the present study, the inhibitory effects of a series of styrylheterocycles having either a p-SO2NH2 or p-SO2Me group on the production of cyclooxygenase-2-mediated PGE2 were evaluated in lipopolysaccharide-stimulated RAW264.7 murine macrophages. Among the series of styrylheterocycle derivatives, (E)-4-(2-(thiophen-3-yl)vinyl)benzenesulfonamide exhibited a potent inhibitory activity, with an IC50 value of 0.013 μM. The inhibitory activity against the overproduction of PGE2 by the active compound was found to be due in part to the suppression of COX-2 mRNA expression.

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