[Adriamycin and its analogs]

Among the biologically active metabolites produced by Streptomyces peucetius adriamycin (syn. doxorubicin) appeared the most effective anthracycline. Because of the low yield of the biosynthetic process, the chemical conversion of daunorubicin to adriamycin represent the key-step of the development of the drug. The therapeutic importance of adriamycin prompted us to begin since 1972 a research program aimed to the development of the second generation anthracyclines. The studies carried out during this research program allowed to discover three new synthetic anthracyclines, which, for the time being, are under clinical investigation: 4'- epidoxorubicin ( epirubicin ), 4-demethoxydaunorubicin ( idarubicin ) and 4'-deoxydoxorubicin ( esorubicin ). These compounds, like daunorubicin and doxorubicin, show affinity to DNA, but some of their pharmacological properties and metabolism in animals as well as in humans are different in respect to those of the parent drugs. Herein the stages of the search for new analogs and the outlooks of further progress in the filed of the antitumor anthracyclines are shortly reported.