Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors

A novel class of PARP-1 inhibitors was identified containing a non-aromatic heterocycle or carbocycle fused to a pyrazolo pyridin-2-one. Compounds displayed low nanomolar binding activity in the PARP-1 binding assay and submicromolar activity in a cell based chemosensitization assay.

Potent PARP-1 inhibitors were identified in a tricyclic pyrazolo pyridine-2-one series with nanomolar binding affinity and submicromar activity in a cell-based chemosensitization assay.Figure optionsDownload as PowerPoint slide