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. 2004 May 17;14(10):2433-7.
doi: 10.1016/j.bmcl.2004.03.017.

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

Alex W White  1 , Nicola J Curtin, Brian W Eastman, Bernard T Golding, Zdenek Hostomsky, Suzanne Kyle, Jianke Li, Karen A Maegley, Donald J Skalitzky, Stephen E Webber, Xiao-Hong Yu, Roger J Griffin
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Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors

Alex W White et al. Bioorg Med Chem Lett. .

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 K(i) 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.

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