Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1364979 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
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
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Keith A. Menear, Claire Adcock, Francisco Cuenca Alonso, Kristel Blackburn, Louise Copsey, Jan Drzewiecki, Alexandra Fundo, Armelle Le Gall, Sylvie Gomez, Hashim Javaid, Carlos Fenandez Lence, Niall M.B. Martin, Chris Mydlowski, Graeme C.M. Smith,