- Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.
Journal of medicinal chemistry (2003-01-10)
Donald J Skalitzky, 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
PMID12519059
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.
MATERIALS