711007-47-5Relevant academic research and scientific papers
SUBSTITUTED 1H-BENZIMIDAZOLE-4-CARBOXAMIDES ARE POTENT PARP INHIBITORS
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Page/Page column 13, (2008/06/13)
Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of For
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.
