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Biguanides drugs: Past success stories and promising future for drug discoveryGrytsai, Oleksandr; Myrgorodska, I.; Rocchi, S.; Ronco, C; Benhida, R.; Université Côte d'Azur, CNRS, Institut de Chimie de Nice UMR 7272, 28 Avenue Valrose, 06108, Nice, France; Drug Discovery Unit, Cancer Research UK Manchester Institute, University of Manchester, Alderley Park, Macclesfield, SK10 4TG, (2021)Biguanides have attracted much attention a century ago and showed resurgent interest in recent years after a long period of dormancy. They constitute an important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases. Therapeutic indications of biguanides include antidiabetic, antimalarial, antiviral, antiplaque, and bactericidal applications. This review presents an extensive overview of the biological activity of biguanides and different mechanisms of action of currently marketed biguanide-containing drugs, as well as their pharmacological properties when applicable. We highlight the recent developments in research on biguanide compounds, with a primary focus on studies on metformin in the field of oncology. We aim to provide a critical overview of all main bioactive biguanide compounds and discuss future perspectives for the design of new drugs based on the biguanide fragment.