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Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization

  作者 DOWLING JAMES E; CHUAQUI CLAUDIO; PONTZ TIMOTHY W; LYNE PAUL D; LARSEN NICHOLAS A; BLOCK MICHAEL H; CHEN HUAWEI; SU NANCY; WU ALLAN; RUSSELL DANIEL; POLLARD HANNAH; LEE JOHN W; PENG BO; THAKUR KUMAR; YE QING; ZHANG TAO; BRASSIL PATRICK; RACICOT VICKI; BAO LARRY; DENZ CHRISTOPHER R; COOKE EMMA  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2012年3-4;  页码  278-283  
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[摘要]In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]-pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described.

 
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