Structure activity relationships of quinoline-containing c-Met inhibitors

Eur J Med Chem. 2008 Jun;43(6):1321-9. doi: 10.1016/j.ejmech.2007.08.011. Epub 2007 Sep 11.

Abstract

A series of quinoline-containing c-Met inhibitors were prepared and studied. Chemistry was developed to introduce a pyridyl moiety onto the 2-aryl ring present in a lead molecule which mitigated the potential for quinone formation relative to the original compound. The study also assessed the importance of an acylthiourea moiety present in the lead structure for effective binding to the c-Met protein ATP site.

MeSH terms

  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology*
  • Proto-Oncogene Proteins c-met / antagonists & inhibitors*
  • Quinolines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Protein Kinase Inhibitors
  • Quinolines
  • quinoline
  • Proto-Oncogene Proteins c-met