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. 2012 Oct 1;22(19):6212-7.
doi: 10.1016/j.bmcl.2012.08.020. Epub 2012 Aug 10.

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

XianYun Jiao  1 , 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
Affiliations

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

XianYun Jiao et al. Bioorg Med Chem Lett. .

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.

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