title: Styrylheterocycles as a novel class inhibitor of cyclooxygenase-2-mediated prostaglandin E(2) production.
abstract: The inhibitory effects of a series of styrylheterocycles on the production of cyclooxygenase-2-mediated prostaglandin E(2) (PGE(2)) were evaluated in lipopolysaccharide-stimulated RAW264.7 murine macrophages. A new series of potential inhibitors, including 3-[2-(4-methoxy-phenyl)-vinyl]-thiophene, have been identified, thus providing novel chemical leads for the further development of potential inhibitors in this capacity. The suppression of COX-2 mRNA expression by the active styrylheterocycles, in part, was involved in the inhibitory activity against the overproduction of PGE(2).
authors.affiliation: College of Pharmacy, Ewha Womans University, 11-1 Daehyun, Seodaemun, Seoul 120-750, South Korea.
authors.forename: Sang Kook
authors.initials: SK
authors.lastname: Lee
authors.forename: Eun-Jung
authors.initials: EJ
authors.lastname: Park
authors.forename: Eunjung
authors.initials: E
authors.lastname: Lee
authors.forename: Hye-Young
authors.initials: HY
authors.lastname: Min
authors.forename: Eun-Young
authors.initials: EY
authors.lastname: Kim
authors.forename: Taeho
authors.initials: T
authors.lastname: Lee
authors.forename: Sanghee
authors.initials: S
authors.lastname: Kim
mesh_terms: D051546:Cyclooxygenase 2; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015232:Dinoprostone / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology*; D007527:Isoenzymes / Q000378:metabolism*; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism*
chemical_list: D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D006571:Heterocyclic Compounds; D007527:Isoenzymes; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases; D015232:Dinoprostone