Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives

Park, H; Dao, TT; Kim, HP

doi:10.1016/j.ejmech.2005.04.013

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Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives

Park, H;
Dao, TT;
Kim, HP

Citations

WEB OF SCIENCE

49

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SCOPUS

54

초록

A series of 6,8-disubstituted chrysin derivatives have been synthesized and evaluated for their PGE(2) inhibitory activities. 6,8-Disubstituted chrysin derivatives were obtained from naturally occurring chrysin by halogenation, oxidation, thiomethylation and C-C cross coupling reaction. Among the compounds investigated, 6,8-dibromochrysin (2), 6,8-diiodochrysin (4), 6,8-dimethylthiochrysin (9) and 6,8-dimethoxychrysin (11) showed as strong inhibitory activities of PGE2 production from LPS-induced RAW 264.7 cells as wogonin, a well known natural flavone having strong and selective COX-2 inhibitory activity. (c) 2005 Elsevier SAS. All rights reserved.

키워드

chrysin; PGE(2) production; anti-inflammatory; COX-2; wogonin; flavonoids; NITRIC-OXIDE SYNTHASE; FACTOR-KAPPA-B; SUPPRESSION; FLAVONOIDS; CELLS; MACROPHAGES; ACTIVATION; EXPRESSION; ANALOGS

제목: Synthesis and inhibition of PGE2 production of 6,8-disubstituted chrysin derivatives

저자: Park, H; Dao, TT; Kim, HP

DOI: 10.1016/j.ejmech.2005.04.013

발행일: 2005-09

유형: Article

저널명: European Journal of Medicinal Chemistry

권: 40

호: 9

페이지: 943 ~ 948