In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors

  • Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61. doi: 10.1016/j.bmcl.2011.03.053.
Tao Wang  1 ,  Stephanos Ioannidis ,  Lynsie Almeida ,  Michael H Block ,  Audrey M Davies ,  Michelle L Lamb ,  David A Scott ,  Mei Su ,  Hai-Jun Zhang ,  Marat Alimzhanov ,  Geraldine Bebernitz ,  Kirsten Bell ,  Michael Zinda
Affiliations
  • 1. Department of Cancer Chemistry, Oncology Innovative Medicines Unit, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. [email protected]
PMID: 21493067 DOI: 10.1016/j.bmcl.2011.03.053
Abstract

Synthesis and biological evaluation of a series of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors was reported. Biochemical screening, followed by profile optimization, resulted in JAK2 inhibitors exhibiting good kinase selectivity, pharmacokinetic properties, physical properties and pharmacodynamic effects.