title: Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation.
abstract: In an effort to develop potent antiplatelet agents, 12 O-prenylated (2-13) and 10 O-allylated (14-23) chalcones were synthesized and screened for in vitro inhibitory effects on aggregation of washed rabbit platelets induced by ADP (20 μM) and collagen (10 μg/mL). In addition, the platelet aggregation activity of previously synthesized Mannich bases of heterocyclic chalcones (MBHC) (24-62) was evaluated. The preliminary structure-activity relationships suggested that the antiplatelet activity was governed to a great extent by the presence of a pyridyl ring-B and a hydroxy group at position C-3' in ring-A of the MBHC templates.
authors: Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan, ROC.
authors: M
authors: M
authors: Vijaya Bhaskar Reddy
authors: Wei-Jern
authors: WJ
authors: Tsai
authors: Keduo
authors: K
authors: Qian
authors: Kuo-Hsiung
authors: KH
authors: Lee
authors: Tian-Shung
authors: TS
authors: Wu
mesh_terms: D000818:Animals; D001792:Blood Platelets / Q000166:cytology / Q000187:drug effects*; D002599:Chalcone / Q000031:analogs & derivatives* / Q000494:pharmacology*; D003094:Collagen / Q000378:metabolism; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011817:Rabbits; D013329:Structure-Activity Relationship
chemical_list: D010975:Platelet Aggregation Inhibitors; D002599:Chalcone; D003094:Collagen