Structure-activity relationship for antineoplastic imidazoacridinones: synthesis and antileukemic activity in vivo.
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).
Cholody
W M
WM
Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdansk, Gdansk, Poland.
Horowska
B
B
Paradziej-Lukowicz
J
J
Martelli
S
S
Konopa
J
J
D000609:Aminoacridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use*; D007941:Leukemia P388 / Q000188:drug therapy*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
C098643:5-((2-((2-(diethylamino)ethyl)amino)ethyl)amino)-8-hydroxy-6H-imidazo(4,5,1-de)acridin-6-one; D000609:Aminoacridines; D000970:Antineoplastic Agents