Synthesis and biological activity of 5-aza-ellipticine derivatives

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2380-4. doi: 10.1016/j.bmcl.2006.09.093.
Deborah L Moody  1 ,  Marcin Dyba ,  Teresa Kosakowska-Cholody ,  Nadya I Tarasova ,  Christopher J Michejda
Affiliations
  • 1. Structural Biophysics Laboratory, Molecular Aspects of Drug Design Section, Structural Biophysics Laboratory, NCI-Frederick, PO Box B Frederick, MD 21702, USA.
PMID: 17376678 DOI: 10.1016/j.bmcl.2006.09.093
Abstract

Novel 5-aza-ellipticine derivatives were synthesized and tested as antitumor agents. The new compounds were prepared more readily than the analogous ellipticine derivatives, which are known to be potent anti-tumor agents Although the novel 5-aza-ellipticine derivatives are not as biologically active as their corresponding ellipticine analogues, the new compounds represent a new, readily accessible class of heteroaromatic catalytic inhibitors of Topoisomerase II and possible anti-tumor agents.