Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2299-304. doi: 10.1016/j.bmcl.2007.01.048. Epub 2007 Jan 24.

Abstract

2,3-Diarylfuro[2,3-b]pyridine-4-amines are a novel class of potent and selective inhibitors of Lck. The discovery, synthesis, and structure activity relationships of this series of inhibitors are reported. The most promising compounds were also profiled to deduce their pharmacokinetic properties.

MeSH terms

  • Amines / chemical synthesis
  • Amines / pharmacokinetics
  • Animals
  • Humans
  • Inhibitory Concentration 50
  • Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
  • Pharmacokinetics
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / pharmacokinetics
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacokinetics*
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship

Substances

  • Amines
  • Protein Kinase Inhibitors
  • Pyridines
  • Lymphocyte Specific Protein Tyrosine Kinase p56(lck)