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J Med Chem. 2003 Jan 16;46(2):210-3.

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

Author information

1
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.

PMID:
12519059
DOI:
10.1021/jm0255769
[Indexed for MEDLINE]

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