A series of styrylquinazoline derivatives (2a-k) were prepared and evaluated for their inhibiton of prostaglandin E(2) (PGE(2)) production by cyclooxygenase-2 (COX-2). The latter was induced by lipopolysaccharide-stimulated macrophage cells RAW264.7. 3', 4'-Dihydroxylated styrylquinazolines (2a-c), 3'-hydroxylated styrylquinazolines (2h, 2i), and 3'-acetoxy-styrylquinazolines (2j, 2k) exhibited good inhibitory effects of PGE(2) production by COX-2 with a range of IC(50) values of 1.19 approximately 3.56 microM. The potencies were comparable or better than that of the representative stilbene resveratrol (IC(50) = 3.07 microM). These results indicate that styrylquinazolines can be considered as potential resveratrol analogues in the modulation of prostaglandin production by COX-2.
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