Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1591-7. doi: 10.1016/j.bmcl.2011.12.130. Epub 2012 Jan 5.

Abstract

PIM kinases have become targets of interest due to their association with biochemical mechanisms affecting survival, proliferation and cytokine production. 1,2,3-Triazolo[4,5-b]pyridines were identified as PIM inhibitors applying a scaffold hopping approach. Initial exploration around this scaffold and X-ray crystallographic data are hereby described.

MeSH terms

  • Drug Design*
  • Enzyme Activation / drug effects
  • Hydrophobic and Hydrophilic Interactions
  • Inhibitory Concentration 50
  • Models, Molecular*
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Proto-Oncogene Proteins c-pim-1 / antagonists & inhibitors*
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Protein Kinase Inhibitors
  • Pyridines
  • Triazoles
  • Proto-Oncogene Proteins c-pim-1
  • proto-oncogene proteins pim