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

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• 作者：James E. Dowling ; Claudio Chuaqui ; Timothy W. Pontz ; Paul D. Lyne ; Nicholas A. Larsen ; Michael H. Block ; Huawei Chen ; Nancy Su ; Allan Wu ; Daniel Russell ; Hannah Pollard ; John W. Lee ; Bo Peng ; Kumar Thakur ; Qing Ye ; Tao Zhang ; Patrick Brassil ; Vicki Racicot ; Larry Bao ; Christopher R. Denz ; Emma Cooke
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：April 12, 2012
• 年：2012
• 卷：3
• 期：4
• 页码：278-283
• 全文大小：378K
• 年卷期：v.3,no.4(April 12, 2012)
• ISSN：1948-5875

文摘

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.

Keywords:

CK2; casein kinase; structure-based design; pyrazolo[1,5-a]pyrimidine