Naphthofuroquinone derivatives: inhibition of receptor tyrosine kinases

Bioorg Med Chem Lett. 2006 Feb;16(3):737-42. doi: 10.1016/j.bmcl.2005.08.115.

Abstract

A series of dinaphtho[1,2-b;2',3'-d]furan-7,12-dione derivatives were synthesized and evaluated for inhibitory activities against receptor tyrosine kinases. The naphthofuroquinone compounds with dialkylaminoethoxy group at C(5)-position (7, 8, 10, and 11) manifested strong inhibitory activities against epidermal growth factor receptor and vascular endothelial growth factor receptor. Docking study of 11 with EGFR was also performed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • ErbB Receptors / antagonists & inhibitors
  • Furans / chemical synthesis*
  • Furans / pharmacology
  • Naphthoquinones / chemical synthesis*
  • Naphthoquinones / pharmacology
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology
  • Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Receptors, Vascular Endothelial Growth Factor / antagonists & inhibitors
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Furans
  • Naphthoquinones
  • Quinazolines
  • ErbB Receptors
  • Receptor Protein-Tyrosine Kinases
  • Receptors, Vascular Endothelial Growth Factor