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 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.
Park
Haeil
H
College of Pharmacy, Kangwon National University, Chuncheon 200-701, South Korea. haeilp@kangwon.ac.kr
Dao
Tran Thanh
TT
Kim
Hyun Pyo
HP
D000818:Animals; D002460:Cell Line; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D015232:Dinoprostone / Q000037:antagonists & inhibitors / Q000378:metabolism*; D004353:Drug Evaluation, Preclinical; D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure
D052246:Cyclooxygenase 2 Inhibitors; D005419:Flavonoids; C043561:chrysin; D015232:Dinoprostone