711007-46-4Relevant articles and documents
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors
White, Alex W.,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,Griffin, Roger J.
, p. 2433 - 2437 (2007/10/03)
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.