Structure-activity relationship for antineoplastic imidazoacridinones: synthesis and antileukemic activity in vivo

J Med Chem. 1996 Mar 1;39(5):1028-32. doi: 10.1021/jm950564r.


Synthesis of several new 5-amino-substituted derivatives of 5-amino-6H-imidazo[4,5,1-de]-acridin-6-one bearing in the benzene ring OH, OCH3, CH3, tert-butyl, or OCH2O groups is described. 8-OH-substituted compounds or double-substituted 7-OH-10-OCH3 compounds demonstrated potent in vivo activity against murine P388 leukemia. The highest activity was exhibited by 5-[[2-[[2-(diethylamino)ethyl]amino]ethyl]amino]-8-hydroxy-6H- imidazo[4,5,1-de]-acridin-6-one (4c).

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoacridines / chemical synthesis*
  • Aminoacridines / chemistry
  • Aminoacridines / therapeutic use*
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / therapeutic use*
  • Leukemia P388 / drug therapy*
  • Magnetic Resonance Spectroscopy
  • Mice
  • Molecular Structure
  • Structure-Activity Relationship


  • 5-((2-((2-(diethylamino)ethyl)amino)ethyl)amino)-8-hydroxy-6H-imidazo(4,5,1-de)acridin-6-one
  • Aminoacridines
  • Antineoplastic Agents