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Synthesis and evaluation of antiplatelet activity of trihydroxychalcone derivatives
Authors:Zhao Li-Ming  Jin Hai-Shan  Sun Liang-Peng  Piao Hu-Ri  Quan Zhe-Shan
Institution:College of Pharmacy, Yanbian University, 121 Juzi Street, Yanji 133000, Jilin, China.
Abstract:In an effort to develop potent antiplatelet agents, a series of trihydroxychalcones was synthesized and screened in vitro for their inhibitory effects on washed rabbit platelet aggregation induced by arachidonic acid (100 microM) and collagen (10 microg/ml). Of five compounds with potent inhibitory effects on arachidonic acid- and collagen-induced platelet aggregation, compound 4e was found to be the most potent. The structure-activity relationships suggested that antiplatelet activity was governed to a greater extent by the substituent on B ring of the chalcone template, and most of the active compounds had methoxy or dimethoxy groups on B ring.
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