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. Epub 2006 Oct 4.

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.

Publication types

  • Research Support, N.I.H., Intramural

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Aza Compounds / chemical synthesis
  • Aza Compounds / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • Ellipticines / chemical synthesis*
  • Ellipticines / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Structure-Activity Relationship
  • Topoisomerase II Inhibitors*

Substances

  • Antineoplastic Agents
  • Aza Compounds
  • Ellipticines
  • Topoisomerase II Inhibitors