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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase
Authors:Menear Keith A  Adcock Claire  Alonso Francisco Cuenca  Blackburn Kristel  Copsey Louise  Drzewiecki Jan  Fundo Alexandra  Le Gall Armelle  Gomez Sylvie  Javaid Hashim  Lence Carlos Fenandez  Martin Niall M B  Mydlowski Chris  Smith Graeme C M
Affiliation:aKuDOS Pharmaceuticals Ltd, 410 Cambridge Science Park, Milton Road, Cambridge CB4 0PE, UK
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.
Keywords:Poly(ADP-ribose) polymerase-1   PARP-1   PARP-2
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