Aminopyrimidinone Cdc7 Kinase Inhibitors

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• 作者：Keith W. Woods ; ^{keith.w.woods@abbott.com} ; Chunqiu Lai ; Julie M. Miyashiro ; Yunsong Tong ; Alan S. Florjancic ; Edward K. Han ; Niru Soni ; Yan Shi ; Loren Lasko ; Joel D. Leverson ; Eric F. Johnson ; Alexander R. Shoemaker ; Thomas D. Penning
• 关键词：Cdc7 ; Kinase ; Pyrimidinone ; Azaindole ; Cancer
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：1 March, 2012
• 年：2012
• 卷：22
• 期：5
• 页码：1940-1943
• 全文大小：1475 K

文摘

We have investigated the SAR of a series of pyrimidinone-containing Cdc7 kinase inhibitors. A wide range of amine substitutions give potent compounds with activities (Kb>ib>) less than 1 nM. Kinase selectivity is reasonable and cytotoxicity corresponds to inhibition of MCM2 phosphorylation.