用噻唑-2-基胺替代吡唑-3-基胺铰链结合物：发现强效和选择性 JAK2 抑制剂。
Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors.
机构信息
Department of Cancer Chemistry, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
出版信息
Bioorg Med Chem Lett. 2010 Mar 1;20(5):1669-73. doi: 10.1016/j.bmcl.2010.01.091. Epub 2010 Jan 25.
PMID:20144546
Abstract
Thiazol-2-yl amine was identified as an isosteric replacement for pyrazol-3-yl amine during our efforts to identify potent and selective JAK2 inhibitors. The rationale, synthesis and biological evaluation of several analogs is reported, along with the in vivo evaluation of the lead compounds.
摘要
在我们努力寻找有效且选择性的 JAK2 抑制剂时，确定噻唑-2-基胺是吡唑-3-基胺的等排体替代物。本文报道了几种类似物的设计、合成和生物学评价，以及先导化合物的体内评估。
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