Synthesis and evaluation of antiplatelet activity of trihydroxychalcone derivatives.
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.
Zhao
Li-Ming
LM
College of Pharmacy, Yanbian University, 121 Juzi Street, Yanji 133000, Jilin, China.
Jin
Hai-Shan
HS
Sun
Liang-Peng
LP
Piao
Hu-Ri
HR
Quan
Zhe-Shan
ZS
D000818:Animals; D001792:Blood Platelets / Q000187:drug effects* / Q000502:physiology; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
D010975:Platelet Aggregation Inhibitors; D002599:Chalcone