title: Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.
abstract: A series of 2'-hydroxychalcones has been synthesized and screened for their in vitro inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin production from lipopolysaccharide-treated RAW 264.7 cells. Structure-activity relationship study suggested that inhibitory activity against prostaglandin E(2) production was governed to a greater extent by the substituent on B ring of the chalcone, and most of the active compounds have at least two methoxy or benzyloxy groups on B ring. The relationship between chalcone structures and their PGE(2) inhibitory activities was also interpreted by docking study on cyclooxygenase-2.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City, Viet Nam.
authors.forename: Thanh-Dao
authors.initials: TD
authors.lastname: Tran
authors.forename: Haeil
authors.initials: H
authors.lastname: Park
authors.forename: Hyun Pyo
authors.initials: HP
authors.lastname: Kim
authors.forename: Gerhard F
authors.initials: GF
authors.lastname: Ecker
authors.forename: Khac-Minh
authors.initials: KM
authors.lastname: Thai
mesh_terms: D000818:Animals; D002460:Cell Line; D002599:Chalcone / Q000737:chemistry*; D047188:Chalcones / Q000138:chemical synthesis* / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D051546:Cyclooxygenase 2 / Q000378:metabolism; D015232:Dinoprostone / Q000378:metabolism*; D015195:Drug Design; D007249:Inflammation; D020128:Inhibitory Concentration 50; D008070:Lipopolysaccharides / Q000737:chemistry; D051379:Mice; D008956:Models, Chemical; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D047188:Chalcones; D008070:Lipopolysaccharides; D002599:Chalcone; D051546:Cyclooxygenase 2; D015232:Dinoprostone; C013031:2'-hydroxychalcone