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Breast cancer is one of the most prevalent malignant diseases and one of the main mortality causes among women across the world. Despite advances in chemotherapy, drug resistance remains major clinical concerns, creating an urgent need to explore novel anti-breast cancer drugs. 1,2,3-Triazole is a privileged moiety, and its derivatives could inhibit cancer cell proliferation, and induce the cell cycle arrest and apoptosis. Accordingly, 1,2,3-triazole derivatives possess profound activity against various cancers including breast cancer. This review summarizes the latest progresses related to the anti-breast cancer potential of 1,2,3-triazole derivatives, covering articles published from January 2017 to December 2021. The mechanisms of action and structure-activity relationships (SARs) are also discussed for further rational design of more effective candidates.

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