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Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035)

Lookup NU author(s): Martin Stockley, Emeritus Professor Bill CleggORCiD, Emeritus Professor Bernard Golding, Nicola Martin, Dr Laurent Rigoreau, Professor Roger Griffin

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Abstract

The first reported synthesis of the DNA-PK inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035) is described. The structure of OK-1035 was validated by X-ray crystallography. An IC50 value of 100 muM was determined for inhibition of DNA-PK, and this is approximately 12-fold higher than that reported previously. (C) 2001 Elsevier Science Ltd. All rights reserved.

Publication metadata

Author(s): Stockley M, Clegg W, Fontana G, Golding BT, Martin N, Rigoreau LJM, Smith GCM, Griffin RJ

Publication type: Article

Publication status: Published

Journal: Bioorganic & Medicinal Chemistry Letters

Year: 2001

Volume: 11

Issue: 21

Pages: 2837-2841

ISSN (print):

ISSN (electronic): 1464-3405

Publisher: Pergamon

URL: http://dx.doi.org/10.1016/S0960-894X(01)00537-6

DOI: 10.1016/S0960-894X(01)00537-6

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