Abstract: N-2-chloroalkyl nitrosouredio derivatives of anthracycline-based compounds having antitumor activity are disclosed. Relative to the clinically-used drugs adriamycin and daunorubicin, substantially enhanced antitumor activity against parent murine P388 leukemia and an adriamycin-resistant P388 leukemia subline has been found for the N-2-chloroethylnitrosoureido derivatives of adriamycin, daunorubicin and epirubicin. Chemical stability has been found to be enhanced when employing the 4'-epi stereoisomeric family of these compounds.