DERIVATIVES OF 3'-AZIRIDIN ANTHRACYCLINE

摘要

Anthracycline glycosides of general formula 1 and 2: IMAGE 1 IMAGE 2 wherein R1 is hydrogen or a methoxy group; R2 is hydrogen, a hydroxy group or represents an acyloxy residue of formula 3 -O-COR5 wherein R5 is a linear or branched C1-C8 alkyl, an aryl group or a heterocyclic mono or bicyclic ring, each of which may be unsubstituted or substituted with (a) an amino group NR6R7 in which R6 and R7 are independently hydrogen or C1-C4 alkyl or (b) a carboxy group; R3 and R4 both represent hydrogen or one of R3 and R4 is hydrogen and the other is hydroxy group or a group of formula -OSO2R8 in which R8 may be a linear or branched alkyl group containing from 1 to 6 carbon atoms or an aryl group unsubstituted or substituted by 1 to 3 substituents each of which may independently be a linear or branched alkyl or alkoxy group of from 1 to 6 carbon atoms, a halogen atom or a nitro group; and pharmaceutically acceptable salts thereof; are active as antitumor agents.