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

Research output: Contribution to journalArticlepeer-review

14 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)7711-7719
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number24
DOIs
Publication statusPublished - 2011 Dec 15

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Structure-activity relationships of chalcone analogs as potential inhibitors of ADP- and collagen-induced platelet aggregation'. Together they form a unique fingerprint.

Cite this