Identification and optimization of N-3,N-6-diaryl-1H-pyrazolo[3,4-d] pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors

[摘要]：A new series of pyrazolo[3,4-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 pro. led for their pharmacokinetic properties. (C) 2008 Elsevier Ltd. All rights reserved.

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