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Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors

Lookup NU author(s): Sara Payne, Sonsoles Rodriguez-Aristegui, Dr Celine Cano, Professor Bernard Golding, Dr Ian Hardcastle, Professor Roger Griffin

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Abstract

Replacement of the core heterocycle of a defined series of chromen-4-one DNA-PK inhibitors by the isomeric chromen-2-one (coumarin) and isochromen-1-one (isocoumarin) scaffolds was investigated. Structure-activity relationships for DNA-PK inhibition were broadly consistent, albeit with a reduction of potency compared with the parent chromenone. (C) 2010 Elsevier Ltd. All rights reserved.


Publication metadata

Author(s): Payne SL, Rodriguez-Aristegui S, Bardos J, Cano C, Golding BT, Hardcastle IR, Peacock M, Parveen N, Griffin RJ

Publication type: Article

Publication status: Published

Journal: Bioorganic & Medicinal Chemistry Letters

Year: 2010

Volume: 20

Issue: 12

Pages: 3649-3653

Print publication date: 14/05/2010

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405

Publisher: Pergamon

URL: http://dx.doi.org/10.1016/j.bmcl.2010.04.102

DOI: 10.1016/j.bmcl.2010.04.102


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