Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

James W. Janetka, Lynsie Almeida, Susan Ashwell, Patrick J. Brassil, Kevin Daly, Chun Deng, Thomas Gero, Roberta E. Glynn, Candice L. Horn, Stephanos Ioannidis, Paul Lyne, Nicholas J. Newcombe, Vibha B. Oza, Martin Pass, Stephanie K. Springer, Mei Su, Dorin Toader, Melissa M. Vasbinder, Dingwei Yu, Yan YuSonya D. Zabludoff

Research output: Contribution to journalArticlepeer-review

30 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)4242-4248
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number14
DOIs
StatePublished - Jul 15 2008

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