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

  • Bioorg Med Chem Lett. 2008 Sep 15;18(18):5126-9. doi: 10.1016/j.bmcl.2008.07.091.
Wilna J Moree  1 ,  Phyllis Goldman ,  Anthony J Demaggio ,  Erik Christenson ,  Dan Herendeen ,  John Eksterowicz ,  Edward A Kesicki ,  David L McElligott ,  Graham Beaton
Affiliations
  • 1. Deltagen Research Laboratories (Former CombiChem, Inc.), 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. [email protected]
PMID: 18713665 DOI: 10.1016/j.bmcl.2008.07.091
Abstract

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.