Journal of Medicinal Chemistry · 2002 · 152 citations · 4 references
MedicineMedicinal ChemistryPharmacologyCancer PharmacologyChemotherapyMolecular OncologyDna Polymerase FunctionEnzyme InhibitionMolecular Targets Of DrugsPolymerase Chain ReactionTopoisomerase InhibitorsDna Damage InductionDna Damage-induced Cell DeathParp InhibitionPoly Adp-ribose Polymerase InhibitorsPoly(adp-ribose) Polymerase 1Poly(adp-ribose) Polymerase ActivityPoly(adp-ribose) Polymerase InhibitionPoly(adp-ribose) Polymerase Inhibitors
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.
4
Alex W. White, Robert J. Almassy, A. Hilary Calvert et al. · Journal of Medicinal Chemistry · 2000 · 287 citations · Full text
Medicine, Oncology, Pharmacology +16
Bruce E. Maryanoff, Winston Ho, David F. McComsey et al. · Journal of Medicinal Chemistry · 1995 · 61 citations