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. Epub 2008 Jul 27.

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.

MeSH terms

  • Animals
  • Chickens
  • Combinatorial Chemistry Techniques
  • Drug Design
  • Enzyme Inhibitors* / chemical synthesis
  • Enzyme Inhibitors* / chemistry
  • Enzyme Inhibitors* / pharmacology
  • Molecular Structure
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Pyrazoles* / chemical synthesis
  • Pyrazoles* / chemistry
  • Pyrazoles* / pharmacology
  • Pyridones* / chemical synthesis
  • Pyridones* / chemistry
  • Pyridones* / pharmacology
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Pyrazoles
  • Pyridones