Styrylheterocycles as a novel class inhibitor of cyclooxygenase-2-mediated prostaglandin E(2) production.
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).
Lee
Sang Kook
SK
College of Pharmacy, Ewha Womans University, 11-1 Daehyun, Seodaemun, Seoul 120-750, South Korea.
Park
Eun-Jung
EJ
Lee
Eunjung
E
Min
Hye-Young
HY
Kim
Eun-Young
EY
Lee
Taeho
T
Kim
Sanghee
S
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*
D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D006571:Heterocyclic Compounds; D007527:Isoenzymes; D051546:Cyclooxygenase 2; D011451:Prostaglandin-Endoperoxide Synthases; D015232:Dinoprostone