4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 14, Pages 4242-4248

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.05.016

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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. (C) 2008 Elsevier Ltd. All rights reserved.

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