Author/Authors :
Keith A. Menear، نويسنده , , Claire Adcock، نويسنده , , Francisco Cuenca Alonso، نويسنده , , Kristel Blackburn، نويسنده , , Louise Copsey، نويسنده , , Jan Drzewiecki، نويسنده , , Alexandra Fundo، نويسنده , , Armelle Le Gall، نويسنده , , Sylvie Gomez، نويسنده , , Hashim Javaid، نويسنده , , Carlos Fenandez Lence، نويسنده , , Niall M.B. Martin، نويسنده , , Chris Mydlowski، نويسنده , , Graeme C.M. Smith، نويسنده ,
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.
