Bergman cyclization of main-chain enediyne polymers for enhanced DNA cleavage

Cai, Y., et al. Polym. Chem., 2022, DOI:

Since the discovery of the role of enediynes in natural antibiotics (such as calicheamicines) via in situ diradical-induced DNA strand cleavage, Bergman cyclization has attracted fervent attention for decades. The synthesis of main-chain enediyne polymers was accomplished, allowing to embed and control the reactivity of the diamino enediynes via polycondensation into polyimines inside their main-chain. These polymers exert a chain-length dependent DNA cleavage activity under physiological conditions, additionally tunable by modulating the stereoelectronic environment via their substitution patterns.