期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 4, 页码 278-283出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml200257n
关键词
CK2; casein kinase; structure-based design; pyrazolo[1,5-a]pyrimidine
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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