Aminopyrimidinone Cdc7 Kinase Inhibitors

作者:Woods Keith W*; Lai Chunqiu; Miyashiro Julie M; Tong Yunsong; Florjancic Alan S; Han Edward K; Soni Niru; Shi Yan; Lasko Loren; Leverson Joel D; Johnson Eric F; Shoemaker Alexander R; Penning Thomas D
来源:Bioorganic & Medicinal Chemistry Letters, 2012, 22(5): 1940-1943.
DOI:10.1016/j.bmcl.2012.01.041

摘要

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 (K-i) less than 1 nM. Kinase selectivity is reasonable and cytotoxicity corresponds to inhibition of MCM2 phosphorylation.

  • 出版日期2012-3-1