After the assessment of the antitumor activity of the anthracycline pigments, the S peucetius group of metabolites was discovered and eventually doxorubicin, a major anticancer agent of established clinical usefulness was developed in the early seventies. A second generation of compounds followed, represented mainly by the better tolerated epirubicin and by the highly potent antileukemic drug, idarubicin. This was the result of a wide program of analog development that provided the basis for further investigations concerning both the study of structure-activity relationships and the synthesis of novel promising derivatives including the 8- and 10-fluoro compounds and the disaccharides. A member of the latter group, namely 7-O-(4'-O-alpha-L-daunosaminyl-2'-deoxy- alpha-L-fucosyl)-4-demethoxyadriamycinone, is undergoing clinical trials as a third generation antitumor anthracycline.