Aza and diaza bioisosteric anthracene-9,10-diones as antitumor agents.

  • A P Krapcho Department of Chemistry, University of Vermont, Burlington 05405, USA.;
  • M J Maresch
  • M P Hacker
  • E Menta
  • A Oliva
  • F C Giuliani
  • S Spinelli

Abstract

Synthetic routes to aza and diaza bioisosteres related to the anthracene-9,10-dione, mitoxantrone, have been developed. The antitumor properties of these chemotypes are compared with those exhibited by the corresponding carbocyclic analogues. The sensitivity of the expressed cytotoxicities on the position(s) of the nitrogen atom(s) are discussed in terms of potential cellular targets. Several analogues show potential for clinical evaluations.
Published
1995-12-31
Section
Articles