Synthesis and biological activity of flavanone derivatives

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5466-8. doi: 10.1016/j.bmcl.2010.07.090. Epub 2010 Jul 25.

Abstract

A series of new flavanone derivatives of farrerol was synthesized by a convenient method. The in vitro anti-tumor activity of these compounds was evaluated against human Bel-7402, HL-60, BGC-823 and KB cell lines, the protein tyrosine kinase (PTK) inhibitor activity was also tested. Their cytoprotective activity was tested using hydrogen peroxide (H2O2)-induced injury in human umbilical vein endothelial cells. Their in vitro anti-atherosclerosis activity was tested on vascular smooth muscle cells by the MTT method using tetrandrine as a positive contrast drug. The structures of all compounds synthesized were confirmed by 1H, 13C NMR and ESI-MS. Most of the compounds exhibited good pharmacological activity and the preliminary structure-activity relationships were described.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Atherosclerosis / drug therapy
  • Cell Line
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cytoprotection / drug effects
  • Endothelial Cells / drug effects
  • Flavanones / chemical synthesis
  • Flavanones / chemistry*
  • Flavanones / pharmacology*
  • Humans
  • Muscle, Smooth, Vascular / cytology
  • Myocytes, Smooth Muscle / drug effects
  • Neoplasms / drug therapy
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Protein-Tyrosine Kinases / metabolism
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Flavanones
  • Protein-Tyrosine Kinases
  • flavanone