Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.
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.
Tran
Thanh-Dao
TD
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.
Park
Haeil
H
Kim
Hyun Pyo
HP
Ecker
Gerhard F
GF
Thai
Khac-Minh
KM
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
D047188:Chalcones; D008070:Lipopolysaccharides; D002599:Chalcone; D051546:Cyclooxygenase 2; D015232:Dinoprostone; C013031:2'-hydroxychalcone