bis-Mannich bases of styryl ketones as antileukemic agents.
A novel series of bis-Mannich bases have been synthesized and evaluated against P388 lymphocytic leukemia in mice. Two compounds showed a perceptible beneficial response in this screen and all the compounds displayed marked murine toxicity. A representative compound inhibited respiration in mitochondria isolated from rat and mouse liver cells by 90% approximately at a dose of 2.5 mumol and it caused a small elevation in mouse liver glutathione equivalent concentrations at 5 mg/kg.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity; D005978:Glutathione / Q000032:analysis; D007941:Leukemia P388 / Q000188:drug therapy*; D007942:Leukemia, Experimental / Q000188:drug therapy*; D008297:Male; D008352:Mannich Bases / Q000138:chemical synthesis / Q000627:therapeutic use; D051379:Mice; D051381:Rats; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity
D000970:Antineoplastic Agents; D008352:Mannich Bases; D013343:Styrenes; D005978:Glutathione