Synthesis and antiproliferative activity of some novel benzo-fused imidazo[1,8]naphthyridinones

  • Bioorg Med Chem Lett. 2015 Jul 1;25(13):2621-3. doi: 10.1016/j.bmcl.2015.04.093.
Vassiliki Giannouli  1 Ioannis K Kostakis  1 Nicole Pouli  2 Panagiotis Marakos  1 Pinelopi Samara  3 Ourania Tsitsilonis  3
Affiliations
  • 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Athens 15771, Greece.
  • 2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Athens, Panepistimiopolis-Zografou, Athens 15771, Greece. Electronic address: [email protected].
  • 3. Department of Animal & Human Physiology, Faculty of Biology, University of Athens, Panepistimiopolis, Athens 15784, Greece.
Abstract

A number of new substituted fused naphthyridinones has been prepared and their antiproliferative activity was evaluated against a panel of seven human tumor cell lines, including the variant MES-SA/Dx5, reported to be 100-fold resistant to doxorubicin. Certain derivatives exhibited interesting cytotoxic properties, possessing IC50 values in a low μM range.

Keywords
Acridines; Cytotoxicity; Imidazonaphthyridinones; Multi-drug resistance.