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Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors |
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| Authors: | Skalitzky Donald J Marakovits Joseph T Maegley Karen A Ekker Anne Yu Xiao-Hong Hostomsky Zdenek Webber Stephen E Eastman Brian W Almassy Robert Li Jianke Curtin Nicola J Newell David R Calvert A Hilary Griffin Roger J Golding Bernard T |
| Affiliation: | Pfizer Global R&D, La Jolla/Agouron Pharmaceuticals, Inc., San Diego, California 92121, USA. |
| 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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