Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors based on a tetrahydro-1(2H)-isoquinolinone scaffold: Synthesis, biological evaluation and X-ray crystal structure

摘要

The synthesis, activity and physical properties of two series of novel potent tetrahydro-1(2H)-isoquinolinone based PARP-1 inhibitors are described. The new structural classes with a non-planar ring system interact specifically with the PARP-1 protein at the nicotinamide-binding site.