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

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

Affiliation

  • 1 Department of Cancer Chemistry, Oncology Innovative Medicines Unit, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA. tao.wang@astrazeneca.com
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.

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