氨嘧啶酮类 CDC7 激酶抑制剂。
Aminopyrimidinone cdc7 kinase inhibitors.
机构信息
Abbott Laboratories, 100 Abbott Park Rd., R47S AP10/307, Abbott Park, IL 60064-6101, USA.
出版信息
Bioorg Med Chem Lett. 2012 Mar 1;22(5):1940-3. doi: 10.1016/j.bmcl.2012.01.041. Epub 2012 Jan 25.
PMID:22326396
Abstract
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 1nM. Kinase selectivity is reasonable and cytotoxicity corresponds to inhibition of MCM2 phosphorylation.
摘要
我们研究了一系列含嘧啶酮的 Cdc7 激酶抑制剂的 SAR。广泛的胺取代可得到活性（K(i)）低于 1nM 的有效化合物。激酶选择性合理，细胞毒性与 MCM2 磷酸化抑制相对应。
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