发现5-（1H-吲哚-5-基）-1,3,4-噻二唑-2-胺作为有效的PIM抑制剂。
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.
作者信息
Wu Bin, Wang Hui-Ling, Cee Victor J, Lanman Brian A, Nixey Thomas, Pettus Liping, Reed Anthony B, Wurz Ryan P, Guerrero Nadia, Sastri Christine, Winston Jeff, Lipford J Russell, Lee Matthew R, Mohr Christopher, Andrews Kristin L, Tasker Andrew S
机构信息
Department of Therapeutic Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA.
Department of Therapeutic Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA.
出版信息
Bioorg Med Chem Lett. 2015 Feb 15;25(4):775-80. doi: 10.1016/j.bmcl.2014.12.091. Epub 2015 Jan 7.
PIM kinases are a family of Ser/Thr kinases that are implicated in tumorigenesis. The discovery of a new class of PIM inhibitors, 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines, is discussed with optimized compounds showing excellent potency against all three PIM isoforms.
PIM激酶是一类与肿瘤发生有关的丝氨酸/苏氨酸激酶。本文讨论了一类新型PIM抑制剂——5-(1H-吲哚-5-基)-1,3,4-噻二唑-2-胺的发现，其中优化后的化合物对所有三种PIM亚型均显示出优异的活性。
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