Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors
Journal of Medicinal Chemistry2002Vol. 46(2), pp. 210–213
Citations Over TimeTop 10% of 2002 papers
Donald J. Skalitzky, Joseph Marakovits, Karen A. Maegley, Anne Ekker, Xiaohong Yu, Zdeněk Hostomský, Stephen E. Webber, Brian Eastman, Robert J. Almassy, Jianke Li, Nicola J. Curtin, David R. Newell, A. Hilary Calvert, Roger J. Griffin, Bernard T. Golding
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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