Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents

  • Eur J Med Chem. 2011 Jun;46(6):2117-31. doi: 10.1016/j.ejmech.2011.02.065.
Constance Genès  1 ,  Gaëlle Lenglet ,  Sabine Depauw ,  Raja Nhili ,  Soizic Prado ,  Marie-Hélène David-Cordonnier ,  Sylvie Michel ,  François Tillequin ,  François-Hugues Porée
Affiliations
  • 1. Université Paris Descartes, Laboratoire de Pharmacognosie, UMR CNRS 8638, 4 Avenue de l'Observatoire, F-75270 Paris Cedex 06, France.
PMID: 21435753 DOI: 10.1016/j.ejmech.2011.02.065
Abstract

Benzo[c]phenanthrolines and benzo[c]phenanthrolinones substituted by dialkylaminoalkyl side chains at position N5 and C6, respectively, were synthesised and their biological activity evaluated. They displayed interessant cytotoxicity associated with some DNA interactions. However, the low Topoisomerase 1 affinity suggests that Other cellular targets are responsible for the antiproliferative activity.