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8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK)

Lookup NU author(s): Dr Celine CanoORCiD, Emeritus Professor Bernard Golding, Dr Ian HardcastleORCiD, Professor Nicola CurtinORCiD, Professor Roger Griffin

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Abstract

The synthesis and biological evaluation of libraries of 8-biarylchromen-4-ones enabled the elucidation of structure-activity relationships for inhibition of the DNA-dependent protein kinase (DNA-PK), with 8-(3-(thiophen-2-yl)phenyl)chromen-4-one and 8-(3-(thiophen-3-yl)phenyl)chromen-4-one being especially potent inhibitors. © 2008 Elsevier Ltd. All rights reserved.

Publication metadata

Author(s): Murr M, Cano C, Golding BT, Hardcastle IR, Hummersome M, Frigerio M, Curtin NJ, Menear K, Richardson C, Smith G, Griffin R

Publication type: Article

Publication status: Published

Journal: Bioorganic and Medicinal Chemistry Letters

Year: 2008

Volume: 18

Issue: 17

Pages: 4885-4890

Date deposited: 29/04/2010

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405

Publisher: Pergamon

URL: http://dx.doi.org/10.1016/j.bmcl.2008.07.066

DOI: 10.1016/j.bmcl.2008.07.066

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