2. Academic Validation
  3. Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors

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

  • J Med Chem. 2003 Jan 16;46(2):210-3. doi: 10.1021/jm0255769.
Donald J Skalitzky 1,  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
Affiliations

Affiliation

  • 1 Pfizer Global R&D, La Jolla/Agouron Pharmaceuticals, Inc., San Diego, California 92121, USA.
PMID: 12519059 DOI: 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.

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