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Styrylquinazolines: A New Class of Inhibitors on Prostaglandin E 2 Production in Lipopolysaccharide‐activated Macrophage Cells
Author(s) -
Park Jang Hyun,
Min HyeYoung,
Kim Sun Suk,
Lee Jae Yeol,
Lee Sang Kook,
Lee Yong Sup
Publication year - 2004
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200300791
Subject(s) - lipopolysaccharide , chemistry , prostaglandin e , prostaglandin , resveratrol , cyclooxygenase , prostaglandin e2 , macrophage , prostaglandin f , pharmacology , biochemistry , stereochemistry , enzyme , in vitro , endocrinology , biology
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 ∼ 3.56 μM. The potencies were comparable or better than that of the representative stilbene resveratrol (IC 50 = 3.07 μM). These results indicate that styrylquinazolines can be considered as potential resveratrol analogues in the modulation of prostaglandin production by COX‐2.