Styrylquinazolines: A new class of inhibitors on prostaglandin E-2 production in lipopolysaccharide-activated macrophage cells

Abstract

4'-Dihydroxylated styrylquinazolines (2 a-c), 3'-hydroxylated styrylquinazolines 3', (2 h, 2 i), and 3'-acetoxy-styrylquinazolines (2 j, 2 k) exhibited good inhibitory effects of PGE(2) production by COX-2 with a range of IC50 values of 1.19 similar to 3.56 muM. The potencies were comparable or better than that of the representative stilbene resveratrol (IC50 = 3.07 muM). These results indicate that styrylquinazolines can be considered as potential resveratrol analogues in the modulation of prostaglandin production by COX-2.