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Review
. 2020 Jul 19;12(7):1959.
doi: 10.3390/cancers12071959.

Coumarins and Coumarin-Related Compounds in Pharmacotherapy of Cancer

Esra Küpeli Akkol  1 , Yasin Genç  2 , Büşra Karpuz  1 , Eduardo Sobarzo-Sánchez  3   4 , Raffaele Capasso  5
Affiliations
Review

Coumarins and Coumarin-Related Compounds in Pharmacotherapy of Cancer

Esra Küpeli Akkol et al. Cancers (Basel). .

Abstract

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.

Keywords: Benzopyrone; cancer; coumarin; drug discovery; natural product.

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Conflict of interest statement

There are no conflicts to declare.

Figures

Figure 1
Figure 1
Chemical structures of some simple coumarins.
Figure 2
Figure 2
Chemical structures of some furanocoumarins.
Figure 3
Figure 3
Chemical structures of some pyranocoumarins.
Figure 4
Figure 4
Chemical structures of some pyrone-substituted coumarins.
Figure 5
Figure 5
Schematic representation of cancer mechanism involving oncogenes (genes such as RAS, Erk and MYC), tumor suppressor genes (TP53 gene) and DNA repair genes.
Figure 6
Figure 6
Basic mechanism of carcinogenesis.
Figure 7
Figure 7
Roles of coumarins in anticancer activity with structure activity relationship.
See this image and copyright information in PMC

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