Synthesis and biological evaluation of dialkylaminoalkylamino benzo[c][1,7] and [1,8]phenanthrolines as antiproliferative agents

  • Eur J Med Chem. 2010 Jun;45(6):2547-58. doi: 10.1016/j.ejmech.2010.02.043.
Tuba Serbetçi  1 ,  Constance Genès ,  Sabine Depauw ,  Soizic Prado ,  François-Hugues Porée ,  Marie-Paule Hildebrand ,  Marie-Hélène David-Cordonnier ,  Sylvie Michel ,  François Tillequin
Affiliations
  • 1. Laboratoire de Pharmacognosie de l'Université Paris Descartes, U.M.R./C.N.R.S. n degrees 8638, Faculté de Pharmacie, 4 Avenue de l'Observatoire, 75006 Paris, France.
PMID: 20236738 DOI: 10.1016/j.ejmech.2010.02.043
Abstract

Benzo[c][1,7] and [1,8]phenanthroline substituted by dialkylaminoalkyl side chains at position C2 and C1, respectively, were synthesized and their biological activity evaluated. These compounds displayed more potent cytotoxicity toward L1210 cells than the parent unsubstituted compounds, associated with strong DNA interaction. The moderate TopoI inhibitory activity induced by the novel compounds suggests that Other cellular targets should be responsible for the antiproliferative activity.