The physiological importance of proteins that can regulate ion balance and transmembrane transport is highlighted by different
diseases where ion channel dysfunction is observed. During the past two decades, considerable effort has been devoted to develop synthetic
ionophores that can insert or cross cell membranes and restore the dysfunction of highly complex protein channels.
Not withstanding the remarkable structural advances made, only a few classes of synthetic ionophores were studied in complex with proand
eukaryote cells in order to obtain information about their biological activity and potential application in ion channel replacement
therapy, anti-cancer therapy or antimicrobial treatments. However, only a few synthetic ionophores showed promising biological activity
in cellular assays. This review aims to show the utility of synthetic ionophores for different biological applications, including: restoring
ion concentration, inducing cell death in different cancer cells, and protecting against a variety of pathogenic microbes. Because the activities
of these ionophores depend primarily on their overall physicochemical properties and structure, we discuss here specific functional
units and scaffolds that are important for obtaining selective, non-toxic transporters for specific biological applications.