Synthesis and biological activity of 6-substituted mitosene analogues of the mitomycins.
A series of 1-acetoxymitosene analogues, in which the substituent at C-6 was varied, was prepared by total synthesis and screened for activity against P388 leukemia in mice and induction of lambda phage in Escherichia coli. Among the 6-substituents prepared, none was as effective as the methyl group in conferring biological activity. However, certain N-methylcarbamates were more active than the unsubstituted carbamates.
D000818:Animals; D001435:Bacteriophages / Q000254:growth & development; D055598:Chemical Phenomena; D002621:Chemistry; D004926:Escherichia coli; D005260:Female; D007941:Leukemia P388 / Q000188:drug therapy*; D007942:Leukemia, Experimental / Q000188:drug therapy*; D051379:Mice; D016685:Mitomycin; D008937:Mitomycins / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014775:Virus Activation / Q000187:drug effects
D008937:Mitomycins; D016685:Mitomycin