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Macrocyclic scaffolds are particularly attractive for designing selective G‐quadruplex ligands essentially because, on one hand, they show a poor affinity for the “standard” B‐DNA conformation and, on the other hand, they fit nicely with the external G‐quartets of quadruplexes. Stimulated by the pioneering studies on the cationic porphyrin TMPyP4 and the natural product telomestatin, follow‐up studies have developed, rapidly leading to a large diversity of macrocyclic structures with remarkable‐quadruplex binding properties and biological activities. In this review we summarize the current state of the art in detailing the three main categories of quadruplex‐binding macrocycles described so far (telomestatin‐like polyheteroarenes, porphyrins and derivatives, polyammonium cyclophanes), and in addressing both synthetic issues and biological aspects.