'Minimal' DNA-intercalating agents as anti-tumour drugs: 2-styrylquinoline analogues of amsacrine

Anticancer Drug Des. 1987 Dec;2(3):263-70.

Abstract

A series of analogues of amsacrine have been prepared by replacing the acridine with a variety of other chromophores, in a search for 'minimal' DNA-intercalating anti-tumour agents which might show superior distributive properties as a consequence of lower levels of binding to cellular macromolecules. 2-Styrylquinoline derivatives did show in vivo anti-leukaemic activity, but none of the compounds was superior to amsacrine itself.

MeSH terms

  • Amsacrine / analogs & derivatives*
  • Amsacrine / pharmacology
  • Antineoplastic Agents / pharmacology*
  • DNA / metabolism*
  • Intercalating Agents / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Intercalating Agents
  • Amsacrine
  • DNA