Breast cancer is the most frequent female cancer and one of the leading causes of cancer
death in women. There are many chemotherapy agents available for the treatment of breast cancer.
Still, the current therapeutic options have not fulfilled the desired outcomes, especially for drug-resistant
breast cancer therapy. Thus, there is an urgent need to develop novel anti-breast cancer
agents. Coumarin is ubiquitous in natural and synthetic bioactive compounds, and coumarin derivatives
readily interact with a variety of enzymes and receptors in breast cancer cells. Moreover, the
coumarin-based irosustat as the first-generation steroid sulfatase inhibitor in breast cancer is under
clinical evaluation, revealing the potential of coumarin derivatives as novel anti-breast cancer
agents. This review aims to describe the recent development of natural and synthetic coumarin derivatives
with anti-breast cancer potential, covering the articles published from 2015 to 2020.
Keywords: Coumarin, Natural product, Dimers, Hybrids, Breast cancer, Steroid, Cancer cells.
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