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Structure-activity relationship for antineoplastic imidazoacridinones: synthesis and antileukemic activity in vivo
W M Cholody1, B Horowska, J Paradziej-Lukowicz
1Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdansk, Gdansk, Poland.
Journal of Medicinal Chemistry
|March 1, 1996
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).