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

White, Alex William, Curtin, Nicola J., Eastman, Brian W., Golding, Bernard T., Hostomsky, Zdenek, Kyle, Suzanne, Li, Jianke, Maegley, Karen A., Skalitzky, Donald J., Webber, Stephen E., Yu, Xiao-Hong and Griffin, Roger J. 2004. Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors. Biorganic and Medicinal Chemistry Letters 14 (10) , pp. 2433-2437. 10.1016/j.bmcl.2004.03.017

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Abstract

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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: Elsevier
ISSN: 0960-894X
Last Modified: 04 Jun 2017 07:48
URI: http://orca-mwe.cf.ac.uk/id/eprint/68212

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