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

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 comp...

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Veröffentlicht in:	European journal of medicinal chemistry 2005-09, Vol.40 (9), p.943-948
Hauptverfasser:	PARK, Haeil, TRAN THANH DAO, HYUN PYO KIM
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Cyclooxygenase 2 Inhibitors - chemical synthesis Cyclooxygenase 2 Inhibitors - pharmacology Dinoprostone - antagonists & inhibitors Dinoprostone - metabolism Drug Evaluation, Preclinical Flavonoids - chemical synthesis Flavonoids - chemistry Flavonoids - pharmacology Macrophages - drug effects Medical sciences Mice Molecular Structure Pharmacology. Drug treatments
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Zusammenfassung:	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.
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2005.04.013