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ID: ALA1153311

Journal: Bioorg Med Chem Lett

Title: Inhibitory activity of prostaglandin E2 production by the synthetic 2'-hydroxychalcone analogues: Synthesis and SAR study.

Authors: Tran TD, Park H, Kim HP, Ecker GF, Thai KM.

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.

CiteXplore: 19233646

DOI: 10.1016/j.bmcl.2009.02.001