Novel poly(ADP-ribose) polymerase-1 inhibitors

Bioorg Med Chem Lett. 2012 Jan 1;22(1):222-4. doi: 10.1016/j.bmcl.2011.11.032. Epub 2011 Nov 17.

Abstract

Synthesis and activity of a series of 3-aroyl-derived analogs of novel pyrrolocarbazole 1 as poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors are disclosed.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Carbazoles / chemistry
  • Chemistry, Pharmaceutical / methods
  • DNA Damage
  • Drug Design
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Models, Chemical
  • NAD / chemistry
  • Neoplasms / drug therapy
  • PC12 Cells
  • Poly (ADP-Ribose) Polymerase-1
  • Poly(ADP-ribose) Polymerase Inhibitors*
  • Rats

Substances

  • Antineoplastic Agents
  • Carbazoles
  • Enzyme Inhibitors
  • Poly(ADP-ribose) Polymerase Inhibitors
  • NAD
  • PARP1 protein, human
  • Parp1 protein, rat
  • Poly (ADP-Ribose) Polymerase-1