Background: The anthracene-9,10-dione (anthraquinone) derivatives represent an exceptionally
valuable class in anticancer drug development. An outstanding antitumor potency of the anthracycline
antibiotics attracted the attention of medicinal chemists since the discovery of these chemotypes.
The prominent anthraquinone-based drugs doxorubicin, mitoxantrone as well as more recent
epirubicin, idarubicin, and valrubicin are successfully used in chemotherapy of hematological malignancies
and solid tumors. The anthraquinone core remains a promising scaffold for the search of new
optimized drug candidates.
Objective: In this study, we analyze the progress in discovery and development of antitumor anthracene-
9,10-diones based on patent and journal publications in 2008-2017. The main goal is to dissect
novel chemotypes of anthraquinone derivatives; other important issues such as the success in bioconjugate
chemistry of anthraquinone containing agents as well as the patents on new applications of anthracyclines
are beyond the scope of this review.
Conclusion: A number of newly discovered natural products, the perspective directions for chemical
modifications to optimize the anticancer properties, and novel intracellular targets demonstrate that anthracene-
9,10-diones deserve further in-depth investigation as an important source of drug candidates.