Acryloylamino-salicylanilides as EGFR PTK inhibitors

Bioorg Med Chem Lett. 2006 Jan 15;16(2):469-72. doi: 10.1016/j.bmcl.2005.06.088. Epub 2005 Nov 3.

Abstract

A series of acryloylamino-salicylanilides were synthesized as inhibitors of EGFR PTK. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bonding in salicylanilides is employed to mimic the planar pyrimidine ring of quinazoline EGFR inhibitors. Acrylamido moiety is incorporated to target the Cys-773 of EGFR specifically. Some of the obtained compounds exhibited good activity as EGFR inhibitors.

MeSH terms

  • Crystallography, X-Ray
  • Drug Design
  • ErbB Receptors / antagonists & inhibitors*
  • Models, Molecular
  • Molecular Structure
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Salicylanilides / chemical synthesis
  • Salicylanilides / chemistry
  • Salicylanilides / pharmacology*
  • Structure-Activity Relationship

Substances

  • Salicylanilides
  • ErbB Receptors
  • Protein-Tyrosine Kinases