Bioorganic and Medicinal Chemistry Letters p. 2433 - 2437 (2004)
Update date:2022-08-03
Topics:
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.
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.
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