Synthesis and Structure-Activity Relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR Tyrosine Kinase Inhibitors

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5978-82. doi: 10.1016/j.bmcl.2007.07.071. Epub 2007 Aug 21.

Abstract

Synthesis and structure-activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • ErbB Receptors / antagonists & inhibitors*
  • Nitriles / chemical synthesis
  • Nitriles / chemistry*
  • Nitriles / pharmacology*
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Nitriles
  • Quinolines
  • ErbB Receptors