Synthesis and evaluation of antiplatelet activity of trihydroxychalcone derivatives |
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Authors: | Zhao Li-Ming Jin Hai-Shan Sun Liang-Peng Piao Hu-Ri Quan Zhe-Shan |
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Institution: | College of Pharmacy, Yanbian University, 121 Juzi Street, Yanji 133000, Jilin, China. |
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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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