FROM THE PIGMENTS OF THE ACTINOMYCETES TO 3RD-GENERATION ANTITUMOR ANTHRACYCLINES

After the assessment of the antitumor activity of the anthracycline pi gments, the S peucetius group of metabolites was discovered and eventu ally doxorubicin, a major anticancer agent of established clinical use fulness was developed in the early seventies. A second generation of c ompounds followed, represented mainly by the better tolerated epirubic in and by the highly potent antileukemic drug, idarubicin. This was th e result of a wide program of analog development that provided the bas is for further investigations concerning both the study of structure-a ctivity relationships and the synthesis of novel promising derivatives including the 8- and 10-fluoro compounds and the disaccharides. A mem ber of the latter group, namely 2'-deoxy-alpha-L-fucosyl)-4-demthoxyad riamycinone, is undergoing clinical trials as a third generation antit umor anthracycline. ((C) Societe francaise de bicchimie et biologie mo leculaire/Elsevier, Paris).