Lookup NU author(s): Professor Nicola Curtin,
Professor Bernard Golding,
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.
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
Print publication date: 17/05/2004
ISSN (print): 0960-894X
ISSN (electronic): 1464-3405
PubMed id: 15109627
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