Transforming the Buckyball: Regioselective Synthesis of Water-Soluble [60]Fullerene Derivatives for Biomedical Applications

Water-soluble fullerene derivatives exhibit a wide range of fascinating biological properties, including antioxidant, antiviral, antitumor, antibacterial, and myogenic effects. During the initial stage of research, most of the reported data on the biological activity of fullerenes were obtained using complex, inseparable mixtures of regiomers with a big focus on fullerenols as the most accessible form of water-soluble fullerene-based compounds. However, during the past decade, significant progress has been made in the synthesis of various isomerically pure water-soluble fullerene derivatives, which opens up possibilities for more directed investigations of their biological activity. In this review, we will highlight current methods for the straightforward synthesis of different types of water-soluble fullerene derivatives with well-defined molecular structures. Special attention will be paid to the possibilities of the precise control of the number, types, and positions of functional groups on the fullerene cage. We will also discuss the opportunities for and challenges within the biomedical applications of water-soluble fullerene derivatives.