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

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

Affiliation

  • 1 Deltagen Research Laboratories (Former CombiChem, Inc.), 4570 Executive Drive, Suite 400, San Diego, CA 92121, USA. wmoree@neurocrine.com
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.

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