Synthesis and biological activity of 6-substituted mitosene analogs of the mitomycins

Abstract
A series of 1-acetoxymitosene analogs, 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 [1-acetoxy-7-methoxy-N-methylmitosene]. Certain N-methylcarbamates were more active than the unsubstituted carbamates.