1099657-75-6Relevant articles and documents
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors
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
scheme or table, p. 6352 - 6356 (2009/09/06)
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 profiled for their pharmacokinetic properties.