TY - JOUR
T1 - Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation
AU - Vijaya Bhaskar Reddy, M.
AU - Tsai, Wei Jern
AU - Qian, Keduo
AU - Lee, Kuo Hsiung
AU - Wu, Tian Shung
N1 - Funding Information:
This work was supported by a Grant of National Science Council, Taiwan, Republic of China , and Grant No.( OUA 95-3-2-021 ) from the National Cheng Kung University, Tainan, Taiwan R.O.C awarded to T. S. Wu. This study is supported in part by Taiwan Department of Health Clinical Trial and Research Center of Excellence ( DOH100-TD-B-111-004 ).
PY - 2011/12/15
Y1 - 2011/12/15
N2 - 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.
AB - 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.
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U2 - 10.1016/j.bmc.2011.08.004
DO - 10.1016/j.bmc.2011.08.004
M3 - Article
C2 - 22055718
AN - SCOPUS:82255175514
VL - 19
SP - 7711
EP - 7719
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 24
ER -