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Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries

Lookup NU author(s): Justin John James Leahy, Professor Bernard Golding, Professor Roger Griffin, Dr Ian Hardcastle, Dr Laurent Rigoreau

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Abstract

A solution-phase multiple-parallel synthesis approach was employed for the preparation of 6-, 7- and 8-aryl-substituted chromenone libraries. which were screened as inhibitors of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). These studies resulted in the identification of 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one (NU7441) as a highly potent and selective DNA-PK inhibitor (IC50 = 14nM), exhibiting ATP-competitive inhibition kinetics. (C) 2004 Elsevier Ltd. All rights reserved.


Publication metadata

Author(s): Leahy JJJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GCM

Publication type: Article

Publication status: Published

Journal: Bioorganic & Medicinal Chemistry Letters

Year: 2004

Volume: 14

Issue: 24

Pages: 6083-6087

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405

URL: http://dx.doi.org/10.1016/j.bmcl.2004.09.060

DOI: 10.1016/j.bmcl.2004.09.060

PubMed id: 15546735


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