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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.
Bioorg Med Chem Lett 2008 Jul 15; 18(14):3942-5.BM

Abstract

We have previously described poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a substituted benzyl-phthalazinone scaffold. As an alternative chemical template, a novel series of alkoxybenzamides were developed with restricted conformation through intramolecular hydrogen bond formation; the compounds exhibit low nM enzyme and cellular activity as PARP-1 inhibitors.

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Publisher Full Text (DOI)

Authors+Show Affiliations

Menear KAKuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0PE, UK. kmenear@kudospharma.co.uk
Adcock CNo affiliation info available
Alonso FCNo affiliation info available
Blackburn KNo affiliation info available
Copsey LNo affiliation info available
Drzewiecki JNo affiliation info available
Fundo ANo affiliation info available
Le Gall ANo affiliation info available
Gomez SNo affiliation info available
Javaid HNo affiliation info available
Lence CFNo affiliation info available
Martin NMNo affiliation info available
Mydlowski CNo affiliation info available
Smith GCNo affiliation info available

MeSH

Chemistry, PharmaceuticalDrug DesignEnzyme InhibitorsHeLa CellsHumansHydrogen BondingInhibitory Concentration 50Models, ChemicalMolecular ConformationMolecular StructurePoly (ADP-Ribose) Polymerase-1Poly(ADP-ribose) Polymerase InhibitorsPoly(ADP-ribose) PolymerasesStructure-Activity RelationshipSubstrate Specificity

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18579376
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