Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6524-8. doi: 10.1016/j.bmcl.2009.10.054. Epub 2009 Oct 24.

Abstract

The design, synthesis and biological evaluation of a series of pyrazol-3-ylamino pyrazines as potent and selective JAK2 kinase inhibitors is reported, along with the pharmacokinetic and pharmacodynamic properties of lead compounds.

MeSH terms

  • Animals
  • Dogs
  • Drug Discovery*
  • Humans
  • Janus Kinase 2 / antagonists & inhibitors*
  • Mice
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrazines / chemical synthesis
  • Pyrazines / chemistry
  • Pyrazines / pharmacology*
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Rats
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Protein Kinase Inhibitors
  • Pyrazines
  • Pyrazoles
  • Janus Kinase 2