Article

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

IRBM-Merck Research Laboratories Rome, Via Pontina km 30,600, Pomezia, 00040 Rome, Italy.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 12/2009; 20(2):448-52. DOI:10.1016/j.bmcl.2009.12.002 pp.448-52
Source: PubMed

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.

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Keywords

low nanomolar enzyme potency
 
promising rat PK properties
 
selective PARP-1 inhibitors