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In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors |
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| Authors: | Wang Tao Ioannidis Stephanos Almeida Lynsie Block Michael H Davies Audrey M Lamb Michelle L Scott David A Su Mei Zhang Hai-Jun Alimzhanov Marat Bebernitz Geraldine Bell Kirsten Zinda Michael |
| Affiliation: | a Department of Cancer Chemistry, Oncology Innovative Medicines Unit, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA b Department of Cancer Bioscience, Oncology Innovative Medicines Unit, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA |
| 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. |
| Keywords: | JAK2 kinase inhibitors Myeloproliferative neoplasms |
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