This review summarizes the development of anthracyclines, addressing the impact of structural modifications on antitumour activity, cardiotoxicity, and multidrug resistance.
This review summarizes the development of anthracyclines, highlighting their antitumour efficacy and the ongoing efforts to mitigate limitations such as multidrug resistance and severe cardiotoxicity.
Anthracyclines are ranked among the most effective chemotherapeutics against cancer. They are glycoside drugs comprising the amino sugar daunosamine linked to a hydroxy anthraquinone aglycone, and act by DNA intercalation, oxidative stress generation and topoisomerase II poisoning. Regardless of their therapeutic value, multidrug resistance and severe cardiotoxicity are important limitations of anthracycline treatment that have prompted the discovery of novel analogues. This review covers the most clinically relevant anthracyclines and their development over decades, since the first discovered natural prototypes to recent semisynthetic and synthetic derivatives. These include registered drugs, drug candidates undergoing clinical trials, and compounds under pre-clinical investigation. The impact of the structural modifications on antitumour activity, toxicity and resistance profile is addressed.
Martins-Teixeira et al. (Mon,) conducted a review in Cancer. Anthracyclines was evaluated. This review summarizes the development of anthracyclines, addressing the impact of structural modifications on antitumour activity, cardiotoxicity, and multidrug resistance.