Potential central nervous system antitumor agents. Aziridinylbenzoquinones. 1.
A series of 3,6-substituted 2,5-diaziridinyl-1,4-benzoquinones was prepared as potential CNS antitumor agents. Activity was evaluated in the murine leukemia L1210 system. The diurethane derivative 9 was found to have significant activity in that system as well as in the intraperitoneal P388 and B16 tumor models. Marginal Lewis lung activity was observed. Reproducible activity was seen in the intracerebral L1210 and P388 systems. Multiple cures were observed in the murine ependymoblastoma brain tumor model. The effect of substituent type on aziridinylquinone activity is discussed.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use; D001388:Aziridines / Q000138:chemical synthesis / Q000627:therapeutic use; D001932:Brain Neoplasms / Q000188:drug therapy; D002490:Central Nervous System; D004806:Ependymoma / Q000188:drug therapy; D007939:Leukemia L1210 / Q000188:drug therapy; D007942:Leukemia, Experimental / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy; D011809:Quinones / Q000138:chemical synthesis* / Q000627:therapeutic use
D000970:Antineoplastic Agents; D001388:Aziridines; D011809:Quinones