1. Academic Validation
  2. Synthesis and biological activity of 5-aza-ellipticine derivatives

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

Affiliation

  • 1 Structural Biophysics Laboratory, Molecular Aspects of Drug Design Section, Structural Biophysics Laboratory, NCI-Frederick, PO Box B Frederick, MD 21702, USA.
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.

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