Benzoquinazoline derivatives as new agents affecting DNA processing

Bioorg Med Chem. 2011 Feb 1;19(3):1197-204. doi: 10.1016/j.bmc.2010.12.037. Epub 2010 Dec 19.

Abstract

A new series of benzo[h]quinazoline and benzo[f]quinazoline derivatives was prepared and studied for the biological activity. The compounds carrying a dimethylaminoethyl side chain (6c, 8c and 12) inhibit cell growth. The ability to form a molecular complex with DNA and to interfere with topoII and topoI relaxation activity was evidenced for the most active 6c and 8c, along with the capacity to induce apoptosis on HeLa cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amsacrine / analogs & derivatives
  • Amsacrine / chemistry
  • Amsacrine / pharmacology
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Cell Cycle / drug effects
  • Cell Proliferation / drug effects
  • DNA / chemistry
  • DNA / metabolism*
  • HeLa Cells
  • Humans
  • Male
  • Models, Molecular
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Salmon
  • Topoisomerase I Inhibitors / chemical synthesis*
  • Topoisomerase I Inhibitors / chemistry
  • Topoisomerase I Inhibitors / pharmacology
  • Topoisomerase II Inhibitors / chemical synthesis*
  • Topoisomerase II Inhibitors / chemistry
  • Topoisomerase II Inhibitors / pharmacology

Substances

  • 6-(N-(dimethylamino)ethyl)aminobenzo(f)quinazoline
  • 6-(N-(dimethylamino)ethyl)aminobenzo(h)quinazoline
  • Antineoplastic Agents
  • Quinazolines
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors
  • Amsacrine
  • DNA