Zentrum für Innovation und Technik in Nordrhein-Westfalen

Discovery, Synthesis,and Biological Evaluation of1,3,4,5-Tetrahydro-6 H -pyrano[4,3- c ]isoquinolin-6-one Derivatives as Novel and Highly SelectivePARP1 Inhibitors

Abstract Developing highly selective PARP1 inhibitors is a promising strategy to improve the therapeutic window compared with dual PARP1/2 inhibitors. Through structure-guided design and optimization, we developed (R)-A17, a novel, highly selective PARP1 inhibitor featuring a uni...