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Lookup NU author(s): Justin John James Leahy,
Professor Bernard Golding,
Professor Roger Griffin,
Dr Ian HardcastleORCiD,
Dr Laurent Rigoreau
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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.
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
ISSN (print): 0960-894X
ISSN (electronic): 1464-3405
PubMed id: 15546735
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