Georgetown University

Eugene McPherson

Philip S Schein

This invention discloses 1a- and 7-substituted derivatives of mitosanes containing thiocarbamoyl and glycosyl residues. The compounds possess antibacterial and antitumor activity, with a concomitant reduction in bone marrow toxicity as compared to the parent compounds.

1a-7-substituted derivatives of mitomycin and uses thereof

Compounds of the formula ##STR1## wherein X is halogen; each R independently represents H, a C.sub.1 -C.sub.4 alkyl group, a C.sub.2 -C.sub.4 alkanoyl group, a phosphate group, or a sulfate, sulfonate, or benzoate group with the proviso that no more than one sulfate, sulfonate, or benzoate group is present in said compound; and R' represents R or a carbohydrate residue derived from a carbohydrate having the formula R'OH with the proviso that R' and the R on C-2 or both R groups on C-3 and C-4 together can represent an isopropylidene group; or a pharmaceutically acceptable salt thereof, are disclosed along with methods of synthesizing and using these compounds.

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Forestville, MD, United States of America

Eugene McPherson