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Coumarins and Coumarin-Related Compounds in Pharmacotherapy of Cancer

Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, Etiler 06330, Ankara, Turkey
Department of Pharmacognosy, Faculty of Pharmacy, Hacettepe University, Sıhhiye 06100, Ankara, Turkey
Instituto de Investigación e Innovación en Salud, Facultad de Ciencias de la Salud, Universidad Central de Chile, 8330507 Santiago, Chile
Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago de Compostela, 15782 Santiago de Compostela, Spain
Department of Agricultural Sciences, University of Naples Federico II, 80055 Portici (Naples), Italy
Authors to whom correspondence should be addressed.
Cancers 2020, 12(7), 1959;
Received: 3 July 2020 / Revised: 14 July 2020 / Accepted: 17 July 2020 / Published: 19 July 2020
(This article belongs to the Special Issue Medicinal Plants and Their Active Ingredients in Cancer)
Cancer is one of the most common causes of disease-related deaths worldwide. Despite the discovery of many chemotherapeutic drugs that inhibit uncontrolled cell division processes for the treatment of various cancers, serious side effects of these drugs are a crucial disadvantage. In addition, multi-drug resistance is another important problem in anticancer treatment. Due to problems such as cytotoxicity and drug resistance, many investigations are being conducted to discover and develop effective anticancer drugs. In recent years, researchers have focused on the anticancer activity coumarins, due to their high biological activity and low toxicity. Coumarins are commonly used in the treatment of prostate cancer, renal cell carcinoma and leukemia, and they also have the ability to counteract the side effects caused by radiotherapy. Both natural and synthetic coumarin derivatives draw attention due to their photochemotherapy and therapeutic applications in cancer. In this review, a compilation of various research reports on coumarins with anticancer activity and investigation and a review of structure-activity relationship studies on coumarin core are presented. Determination of important structural features around the coumarin core may help researchers to design and develop new analogues with a strong anticancer effect and reduce the potential side effects of existing therapeutics. View Full-Text
Keywords: Benzopyrone; coumarin; cancer; drug discovery; natural product Benzopyrone; coumarin; cancer; drug discovery; natural product
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Küpeli Akkol, E.; Genç, Y.; Karpuz, B.; Sobarzo-Sánchez, E.; Capasso, R. Coumarins and Coumarin-Related Compounds in Pharmacotherapy of Cancer. Cancers 2020, 12, 1959.

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