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Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors

Lookup NU author(s): Professor Nicola CurtinORCiD, Emeritus Professor Bernard Golding, Suzanne Kyle, Professor Roger Griffin


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The synthesis and biological evaluation of a new series of amine-substituted 2-arylbenzimidazole-4-carboxamide inhibitors of the DNA-repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) is reported. The introduction of an amine substituent at the 2-aryl position is not detrimental to activity, with most inhibitors exhibiting Ki values for PARP-1 inhibition in the low nanomolar range. Two compounds in this series were found to potentiate the cytotoxicity of the DNA-methylating agent temozolomide by 4-5-fold in a human colorectal cancer cell line. © 2004 Published by Elsevier Ltd.

Publication metadata

Author(s): White, A., Curtin, N.J., Eastman, B., Golding, B.T., Hostomsky, Z., Kyle,S., Li, J., Maegley, K., Skalitzky, D., Webber, S., Yu, X., Griffin, R.J.

Publication type: Article

Publication status: Published

Journal: Bioorganic and Medicinal Chemistry Letters

Year: 2004

Volume: 14

Issue: 10

Pages: 2433-2437

Print publication date: 17/05/2004

ISSN (print): 0960-894X

ISSN (electronic): 1464-3405


DOI: 10.1016/j.bmcl.2004.03.017

PubMed id: 15109627


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