Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors

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• 作者：XianYun Jiao ; David J. Kopecky ; JinSong Liu ; JinQian Liu ; Juan C. Jaen ; Mario G. Cardozo ; Rajiv Sharma ; Nigel Walker ; Holger Wesche ; Shyun Li ; Ellyn Farrelly ; Shou-Hua Xiao ; Zhulun Wang ; Frank Kayser
• 关键词：ACK1 ; Cancer ; Tyrosine kinase inhibitor ; Furo[2 ; 3-d]-pyrimidin-4-amine ; 7H-Pyrrolo[2 ; 3-d]pyrimidin-4-amine
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：1 October, 2012
• 年：2012
• 卷：22
• 期：19
• 页码：6212-6217
• 全文大小：3403 K

文摘

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.