期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 12, 页码 4351-4362出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.04.087
关键词
Anaplastic lymphoma kinase; Kinase inhibitors
Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3-b]pyrazines was constructed as ring-constrained analogs of a known aminopyridine kinase scaffold. Chemistry was developed to rapidly elaborate the SAR, structural elements impacting ALK inhibitory activity were exploited, and kinase selective analogs were identified that inhibit ALK with IC50 values similar to 10 nM (enzyme) and similar to 150 nM (cell). (C) 2010 Elsevier Ltd. All rights reserved.
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