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ID: ALA1153250

Journal: Bioorg Med Chem Lett

Title: Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Authors: Torrisi C, Bisbocci M, Ingenito R, Ontoria JM, Rowley M, Schultz-Fademrecht C, Toniatti C, Jones P.

Abstract: A novel hexahydrobenzonaphthyridinone PARP-1 pharmacophore is reported, subsequent SAR exploration around this scaffold led to selective PARP-1 inhibitors with low nanomolar enzyme potency, displaying good cellular activity and promising rat PK properties.

CiteXplore: 20015648

DOI: 10.1016/j.bmcl.2009.12.002