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

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.

DOI: 10.1016/j.bmcl.2012.08.020

Cite this paper

@article{Jiao2012SynthesisAO, title={Synthesis and optimization of substituted furo[2,3-d]-pyrimidin-4-amines and 7H-pyrrolo[2,3-d]pyrimidin-4-amines as ACK1 inhibitors.}, author={Xianyun Jiao and David J Kopecky and Jinsong Liu and Jinqian Liu and Juan C. Jaen and Mario G. Cardozo and Rajiv P. Sharma and Nigel P C Walker and Holger Wesche and Shyun Li and Ellyn R Farrelly and Shou-Hua Xiao and Zhulun Wang and Frank Kayser}, journal={Bioorganic & medicinal chemistry letters}, year={2012}, volume={22 19}, pages={6212-7} }