4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 6, Pages 2117-2131

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.02.065

Keywords

Benzo[c]phenanthrolines; Benzo[c]phenanthrolinones; Dialkylaminoalkyl side chains; Cytotoxicity; DNA interactions

Funding

  1. Universite de Lille 2/Conseil Regional Nord/Pas-de-Calais
  2. Institut pour la Recherche sur le Cancer de Lille (IRCL)
  3. Ligue Nationale Contre le Cancer (Comite du Nord)

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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. (C) 2011 Elsevier Masson SAS. All rights reserved.

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