Antitumor activity of new N-substituted daunorubicin derivatives.

The biological properties of two new structural groups of modification products of daunorubicin, the N-glycosyl and enamino derivatives, were investigated. The activities of the compounds were characterized in vitro (yeasts and leukaemia cells) and in vivo (L1210 leukaemia in mice). Among the compounds studied DR-19, N-(1-carboethoxypropen-1-yl)daunorubicin, exhibited activity comparable with that of the parent antibiotic. The correlation coefficients calculated showed good correlation between in vitro tests. In vitro activity and potency (reciprocal of optimal dose) in mice leukaemia were also correlated. However, no correlation between the in vitro activity and activity in mice leukaemia (increase of life span) was observed.