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

Skalitzky, DJ; Marakovits, JT; Maegley, KA; Ekker, A; Yu, XH; Hostomsky, Z; Webber, SE; ... Golding, BT; + view all (2003) Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J MED CHEM , 46 (2) 210 - 213. 10.1021/jm0255769.

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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 ADPribose polymer formation caused by chemically induced DNA damage.

Type: Article
Title: Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors
DOI: 10.1021/jm0255769
Keywords: RESISTANCE-MODIFYING AGENTS, CYTOTOXICITY, CELLS, MICE
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Cancer Institute
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Cancer Institute > Research Department of Oncology
URI: http://discovery.ucl.ac.uk/id/eprint/351695
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