Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation

M Vijaya Bhaskar Reddy; Wei-Jern Tsai; Keduo Qian; Kuo-Hsiung Lee; Tian-Shung Wu

doi:10.1016/j.bmc.2011.08.004

Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation

Bioorg Med Chem. 2011 Dec 15;19(24):7711-9. doi: 10.1016/j.bmc.2011.08.004. Epub 2011 Aug 6.

Authors

M Vijaya Bhaskar Reddy¹, Wei-Jern Tsai, Keduo Qian, Kuo-Hsiung Lee, Tian-Shung Wu

Affiliation

¹ Department of Chemistry, National Cheng Kung University, Tainan 701, Taiwan, ROC.

PMID: 22055718
DOI: 10.1016/j.bmc.2011.08.004

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Blood Platelets / cytology
Blood Platelets / drug effects*
Chalcone / analogs & derivatives*
Chalcone / pharmacology*
Collagen / metabolism
Platelet Aggregation / drug effects*
Platelet Aggregation Inhibitors / chemistry*
Platelet Aggregation Inhibitors / pharmacology*
Rabbits
Structure-Activity Relationship

Substances

Platelet Aggregation Inhibitors
Chalcone
Collagen