Park Haeil, Dao Tran Thanh, Kim Hyun Pyo
College of Pharmacy, Kangwon National University, Chuncheon 200-701, South Korea.
Eur J Med Chem. 2005 Sep;40(9):943-8. doi: 10.1016/j.ejmech.2005.04.013. Epub 2005 Jun 15.
A series of 6,8-disubstituted chrysin derivatives have been synthesized and evaluated for their PGE2 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.
已合成了一系列6,8-二取代白杨素衍生物，并对其PGE2抑制活性进行了评估。6,8-二取代白杨素衍生物是通过卤化、氧化、硫甲基化和C-C交叉偶联反应从天然存在的白杨素制得的。在所研究的化合物中，6,8-二溴白杨素（2）、6,8-二碘白杨素（4）、6,8-二甲硫基白杨素（9）和6,8-二甲氧基白杨素（11）对脂多糖诱导的RAW 264.7细胞产生PGE2具有与汉黄芩素一样强的抑制活性，汉黄芩素是一种具有强且选择性COX-2抑制活性的著名天然黄酮。
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