期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 11, 页码 3727-3731出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.04.024
关键词
CDC7 kinase inhibitor; CK2 inhibitors; Benzofuropyrimidinone; Cell cycle arrest
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model. (C) 2012 Elsevier Ltd. All rights reserved.
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