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Discrete supramolecular constructs continue to attract important research interest because of their myriad of applications, including in biology. The biomedical application of supramolecular coordination complexes (SCCs) is still an emergent field of study, but the pioneering examples discussed in this chapter confirm that these scaffolds hold promise as novel anticancer drugs, endowed with different mechanisms of action compared to classical small-molecule and metal-based cytotoxic agents, often linked to their peculiar molecular recognition properties. Moreover, the host–guest chemistry of SCCs can also be exploited to design a new generation of drug delivery systems for anticancer chemotherapeutics. In fact, the robustness of supramolecular metal-based complexes allows incorporation of different functionalities in the same scaffold to enable imaging in cells, as well as targeting and stimuli responsiveness. Certainly, the myriad of possible SCCs and their almost limitless modularity and tunability, without significant synthetic penalty, suggests that the biomedical applications of such species will continue along this already promising path. In this chapter, we aim to summarize the main concepts in this fascinating research area, illustrating representative examples and providing a critical discussion of the state-of-the-art.

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