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

Stephanos Ioannidis; Michelle L Lamb; Audrey M Davies; Lynsie Almeida; Mei Su; Geraldine Bebernitz; Minwei Ye; Kirsten Bell; Marat Alimzhanov; Michael Zinda

doi:10.1016/j.bmcl.2009.10.054

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.

Authors

Stephanos Ioannidis¹, Michelle L Lamb, Audrey M Davies, Lynsie Almeida, Mei Su, Geraldine Bebernitz, Minwei Ye, Kirsten Bell, Marat Alimzhanov, Michael Zinda

Affiliation

¹ Department of Cancer Chemistry, AstraZeneca R&D Boston, Waltham, MA 02451, USA. [email protected]

PMID: 19857966
DOI: 10.1016/j.bmcl.2009.10.054

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