Synthesis of some flavone derivatives: potent inhibitors of human platelet aggregation

Ertan R., GÖKER A. H., Ertan M., Beretz A., Cazenave J., Haag M., ...More

European Journal of Medicinal Chemistry, vol.26, no.7, pp.735-738, 1991 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 7
  • Publication Date: 1991
  • Doi Number: 10.1016/0223-5234(91)90124-6
  • Journal Name: European Journal of Medicinal Chemistry
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.735-738
  • Keywords: aggregation, cyclic AMP, flavonoid, human platelet, phosphodiesterase
  • Ankara University Affiliated: Yes

Abstract

A series of 20 benzodioxan derivatives of flavone were synthesized and characterised each bearing an ester or amide side chain of variable length. The activity of the compounds on washed human platelet aggregation induced by ADP (5 μM), collagen (2.5 μg/ml) and thrombin (0.1 U/ml) was evaluated. The ethoxycarbonyl side chain derivative inhibited all 3 types of aggregation agents with an IC50 of 1, 2, and 24 μM respectively, making it one of the most potent platelet aggregation inhibitors among the flavonoids. Its mode of action should involve an increase in platelet cyclic AMP. © 1991.