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

W M Cholody; B Horowska; J Paradziej-Lukowicz; S Martelli; J Konopa

doi:10.1021/jm950564r

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.

Authors

W M Cholody¹, B Horowska, J Paradziej-Lukowicz, S Martelli, J Konopa

Affiliation

¹ Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdansk, Gdansk, Poland.

PMID: 8676337
DOI: 10.1021/jm950564r

Abstract

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

Substances

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