Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors |
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Authors: | Kopecky David J Hao Xiaolin Chen Yi Fu Jiasheng Jiao XianYun Jaen Juan C Cardozo Mario G Liu Jinsong Wang Zhulun Walker Nigel P C Wesche Holger Li Shyun Farrelly Ellyn Xiao Shou-Hua Kayser Frank |
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Institution: | Department of Chemistry, Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. dkopecky@amgen.com |
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Abstract: | A new series of pyrazolo3,4-d]pyrimidine-3,6-diamines was designed and synthesized as potent and selective inhibitors of the nonreceptor tyrosine kinase, ACK1. These compounds arose from efforts to rigidify an earlier series of N-aryl pyrimidine-5-carboxamides. The synthesis and structure-activity relationships of this new series of inhibitors are reported. The most promising compounds were also profiled for their pharmacokinetic properties. |
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