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Selenium (Se) is an essential trace element involved in many fundamental biological processes. Our knowledge about the potential of Se in cancer therapy has expanded greatly in recent years and has opened a new research perspective in the development of selenium-based anticancer agents. Notably, selenium compounds possess a selective activity against tumor cells, and the major mechanisms accounting for this selectivity are the tumor-specific Se uptake and the dysregulation of redox homeostasis in cancer cells. Herein, we summarize the current knowledge on organoselenium compounds endowed with in vitro and/or in vivo antitumor potential.

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