Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors
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- 作者：James W. Janetka ; Lynsie Almeida ; Susan Ashwell ; Patrick J. Brassil ; Kevin Daly ; Chun Deng ; Thomas Gero ; Roberta E. Glynn ; C ; ice L. Horn ; Stephanos Ioannidis ; Paul Lyne ; Nicholas J. Newcombe ; Vibha B.
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 July 2008
- 年：2008
- 卷：18
- 期：14
- 页码：4242-4248
- 全文大小：254 K
文摘
Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.