Tricyclic Benzimidazoles as Potent Poly(ADP-ribose) Polymerase-1 Inhibitors
- 17 December 2002
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 46 (2) , 210-213
- https://doi.org/10.1021/jm0255769
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.Keywords
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