Identification of 3-amido-4-anilinoquinolines as potent and selective inhibitors of CSF-1R kinase

Bioorg Med Chem Lett. 2009 Feb 1;19(3):697-700. doi: 10.1016/j.bmcl.2008.12.046. Epub 2008 Dec 24.

Abstract

3-amido-4-anilinoquinolines are potent and highly selective inhibitors of CSF-1R. Their synthesis and SAR is reported, along with initial efforts to optimize the physical properties and PK through modifications at the quinoline 6- and 7-positions.

MeSH terms

  • Administration, Oral
  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Models, Chemical
  • Neoplasms / drug therapy*
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry
  • Quinolines / chemistry*
  • Quinolines / pharmacokinetics*
  • Rats
  • Receptor, Macrophage Colony-Stimulating Factor / antagonists & inhibitors*
  • Receptor, Macrophage Colony-Stimulating Factor / chemistry*

Substances

  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Quinolines
  • Receptor, Macrophage Colony-Stimulating Factor