Development of a high-contrast fluorescent ligand that targets G-quadruplexes by introducing a triazole rotor onto the dibenzoquinoxaline scaffold.

In this study, we developed a potential dual-function ligand targeting G-quadruplexes (G4s) by introducing a triazole rotor onto the dibenzoquinoxaline scaffold. This ligand not only had potential in high-contrast imaging of G4s either in vitro or in cellulo, but also proved to inhibit cancer cell growth as well as migration possibly through a G4-mediated action of mechanism. Altogether, this ligand had possibility to develop into a theranostic agent for cancer diagnosis and therapy in the future. • A dual-function fluorescent ligand targeting G4s was developed. • The ligand showed high-contrast fluorescence upon interaction with G4s. • The ligand was able to label and stabilize the DNA G4s in live cells. [ABSTRACT FROM AUTHOR]