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Recent Pat Anticancer Drug Discov. 2018;13(2):159-183. doi: 10.2174/1574892813666171206123114.

Advances in the Discovery of Anthraquinone-Based Anticancer Agents.

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Gause Institute of New Antibiotics, 11 B. Pirogovskaya Street, Moscow 119021, Russian Federation.
Mendeleyev University of Chemical Technology, 9 Miusskaya Square, Moscow 125190, Russian Federation.
Blokhin National Medical Center of Oncology, 24 Kashirskoye Shosse, Moscow 115478, Russian Federation.
ITMO University, 49 Kronverksky Avenue, Saint Petersburg 197101, Russian Federation.



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.


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.


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.


Anthraquinone; anticancer agents; chemical modifications; cytotoxicity; intracellular targets; structure-activity relationship.

[Indexed for MEDLINE]

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