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. 2003 Jan 16;46(2):210-3.
doi: 10.1021/jm0255769.

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors

Donald J Skalitzky  1 , Joseph T Marakovits, Karen A Maegley, Anne Ekker, Xiao-Hong Yu, Zdenek Hostomsky, Stephen E Webber, Brian W Eastman, Robert Almassy, Jianke Li, Nicola J Curtin, David R Newell, A Hilary Calvert, Roger J Griffin, Bernard T Golding
Affiliations

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors

Donald J Skalitzky et al. J Med Chem. .

Abstract

Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro inhibition of PARP-1 was confirmed by direct measurement of NAD+ depletion and ADP-ribose polymer formation caused by chemically induced DNA damage.

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