Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase

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.

Graphical abstractA novel series of alkoxybenzamides have been developed with restricted conformation through intramolecular hydrogen bond formation. The compounds exhibit low nM enzyme and cellular activity as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide