6-氨基哒嗪基吡啶-3-甲腈类化合物作为 JAK2 激酶抑制剂的体外和体内评价。
In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
机构信息
Department of Cancer Chemistry, Oncology Innovative Medicines Unit, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
出版信息
Bioorg Med Chem Lett. 2011 May 15;21(10):2958-61. doi: 10.1016/j.bmcl.2011.03.053. Epub 2011 Mar 21.
PMID:21493067
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.
摘要
报道了一系列 6-氨基吡唑基吡啶-3-甲腈作为 JAK2 激酶抑制剂的合成和生物学评价。通过生化筛选，然后进行特征优化，得到了具有良好激酶选择性、药代动力学性质、物理性质和药效学作用的 JAK2 抑制剂。
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