2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors

Bioorg Med Chem Lett. 2013 Sep 1;23(17):5014-21. doi: 10.1016/j.bmcl.2013.06.008. Epub 2013 Jun 15.

Abstract

The advancement of a series of ligand efficient 2-amino-[1,2,4]triazolo[1,5-a]pyridines, initially identified from high-throughput screening, to a JAK2 inhibitor with pharmacodynamic activity in a mouse xenograft model is disclosed.

Keywords: JAK2; Janus kinase; Triazolopyridine.

MeSH terms

  • Amitrole / chemistry*
  • Amitrole / pharmacology
  • Amitrole / therapeutic use*
  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Crystallography, X-Ray
  • Humans
  • Janus Kinase 2 / antagonists & inhibitors*
  • Janus Kinase 2 / chemistry
  • Janus Kinase 2 / metabolism
  • Mice
  • Models, Molecular
  • Neoplasms / drug therapy
  • Neoplasms / enzymology
  • Neoplasms / pathology
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use*
  • Structure-Activity Relationship
  • Triazoles / chemistry*
  • Triazoles / pharmacology
  • Triazoles / therapeutic use*

Substances

  • 1,2,4-triazolo(1,5-c)pyrimidine
  • Antineoplastic Agents
  • Pyrimidines
  • Triazoles
  • Janus Kinase 2
  • Amitrole