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

Lookup NU author(s): Professor Nicola CurtinORCiD, Professor Herbie Newell, Professor Alan Calvert, Professor Roger Griffin, Emeritus Professor Bernard Golding

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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.

Publication metadata

Author(s): Skalitzky, D., Marakovits, J., Maegley, K., Ekker, A., Yu, X., Hostomsky, Z., Webber, S., Eastman, B., Almassy, R., Li, J., Curtin, N. J., Newell, D. R., Calvert, A. H., Griffin, R. J., Golding, B. T.

Publication type: Article

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2003

Volume: 46

Issue: 2

Pages: 210-213

Print publication date: 16/01/2003

ISSN (print): 00222623

ISSN (electronic):

URL: http://dx.doi.org/10.1021/jm0255769

DOI: 10.1021/jm0255769

PubMed id: 12519059

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