Title of article
Identification and optimization of N3,N6-diaryl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamines as a novel class of ACK1 inhibitors
Author/Authors
David J. Kopecky، نويسنده , , Xiaolin Hao، نويسنده , , Yi Chen، نويسنده , , Jiasheng Fu، نويسنده , , XianYun Jiao، نويسنده , , Juan C. Jaen، نويسنده , , Mario G. Cardozo، نويسنده , , Jinsong Liu، نويسنده , , Zhulun Wang، نويسنده , , Nigel P.C. Walker، نويسنده , , Holger Wesche، نويسنده , , Shyun Li، نويسنده , , Ellyn Farrelly، نويسنده , , Shou-Hua Xiao، نويسنده , , Frank Kayser، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
6352
To page
6356
Abstract
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.
Keywords
-d]pyrimidine-3 , 6-diamine , 4 , ACK1 , kinase inhibitor , cancer , SAR
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800234
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