Synthfsis of bis(aziridinyl)phosphinyl-N-hydroxyurethane derivatives as antineoplastic agents.
Several new "dual antagonists" were synthesized in which the 2,2-dimethyl (or ring C unsubstituted) aziridine phosphinyl function is linked to N-hydroxyurethane rather than the urethane moiety. Three of the new compounds showed very high activities against leukemia L1210 in mice.
D000477:Alkylating Agents / Q000138:chemical synthesis; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D001388:Aziridines / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D001389:Azirines / Q000138:chemical synthesis*; D004353:Drug Evaluation, Preclinical; D005260:Female; D007928:Lethal Dose 50; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D010720:Phosphines / Q000138:chemical synthesis / Q000627:therapeutic use / Q000633:toxicity; D014520:Urethane / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use / Q000633:toxicity
D000477:Alkylating Agents; D000970:Antineoplastic Agents; D001388:Aziridines; D001389:Azirines; D010720:Phosphines; D014520:Urethane