Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors

Bioorg Med Chem Lett. 2011 May 1;21(9):2732-5. doi: 10.1016/j.bmcl.2010.11.104. Epub 2010 Dec 1.

Abstract

The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered.

MeSH terms

  • Enzyme Activation / drug effects
  • Inhibitory Concentration 50
  • JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship

Substances

  • Protein Kinase Inhibitors
  • Pyrazoles
  • Pyrimidines
  • pyrazole
  • JNK Mitogen-Activated Protein Kinases