取代的呋喃[2,3-d]-嘧啶-4-胺和 7H-吡咯并[2,3-d]嘧啶-4-胺的合成与优化作为 ACK1 抑制剂。
Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.
机构信息
Department of Medicinal Chemistry, Amgen Inc., 1120 Veterans Blvd., South San Francisco, CA 94080, USA.
出版信息
Bioorg Med Chem Lett. 2012 Oct 1;22(19):6212-7. doi: 10.1016/j.bmcl.2012.08.020. Epub 2012 Aug 10.
PMID:22929232
Abstract
Two classes of ACK1 inhibitors, 4,5,6-trisubstituted furo[2,3-d]pyrimidin4-amines and 4,5,6-trisubstituted 7H-pyrrolo[2,3-d]pyrimidin-4-amines, were discovered and evaluated as ACK1 inhibitors. Further structural refinement led to the identification of potent and selective dithiolane inhibitor 37.
摘要
两类 ACK1 抑制剂，即 4,5,6-三取代的呋喃[2,3-d]嘧啶-4-胺和 4,5,6-三取代的 7H-吡咯并[2,3-d]嘧啶-4-胺，被发现并评估为 ACK1 抑制剂。进一步的结构优化导致了具有强效和选择性的二硫戊环抑制剂 37 的鉴定。
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