Anthracyclines rank among the most effective anticancer agents ever
developed. Nevertheless, the clinical use of anthracyclines can be viewed as a sort of
double-edged sword. On the one hand, anthracycline antibiotics are extensively used in
conventional chemotherapy of solid tumors and hematological malignancies. On the
other hand, the clinical efficacy of the drugs is limited by severe side effects,
particularly cardiotoxicity, and the development of multiple mechanisms of cellular
drug resistance. Therefore, several strategies for improving the efficacy of currently
approved anthracyclines have moved along two medicinal chemistry lines, the
development of both new analogs and cancer cell-targeted formulations. There is still
necessary to develop these new strategies for improving the effectiveness and reducing
side effects of the action of anthracyclines, respectively on cancer and normal cells. The
current available knowledge on anthracyclines is based on a collection of the original
published studies, conference abstracts, and relevant articles.
Keywords: Anthracycline cytotoxicity/cardiotoxicity, anthracyclines, cellular
drug resistance, daunorubicin, doxorubicin, mechanisms of anthracycline
action, new anthracycline analogs, next generation anthracyclines, tumortargeted
formulations.
