Please login first
2’-Hydroxychalcone Analogues: Synthesis and Structure-PGE2 Inhibitory Activity Relationship
* 1 , 2 , 3 , 1, 3
1  Department of Pharmaceutical Chemistry, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City, Vietnam
2  College of Pharmacy, Kangwon National University, Chuncheon 200-701, Republic of Korea
3  Emerging Field Pharmacoinformatics, Department of Medicinal Chemistry, University of Vienna, Althanstrasse 14, A-1090, Vienna, Austria

Abstract: A series of 2’-hydroxychalcones was synthesized and screened for their in vitro inhibitory effects on PGE2 production from RAW 264.7 cells induced by LPS. Structure–activity relationship study suggested that inhibitory activity of PGE2 formation was governed to a greater extent by the substituent on B ring of the chalcone template, and most of the active compounds have at least two methoxyl or benzyloxyl groups on B ring. The relationship between chalcone structures and their PGE2 inhibitory activity was also interpreted by docking study on cyclooxygenase 2.
Keywords: n/a