Development and Characterization of Benzoselenazole Derivatives as Potent and Selective Transcription Inhibitors.

Developing transcription inhibitors that target the G-quadruplex has generated significant interest; however, few compounds have demonstrated specificity for G-quadruplex and cancer cells. In this study, we designed and synthesized a series of benzoazole derivatives as potential G-quadruplex ligand-based transcription inhibitors. Surprisingly, benzoselenazole derivatives, which are rarely reported as G-quadruplex ligands, demonstrated greater G-quadruplex selectivity and cancer cell specificity compared to their benzothiazole and benzoxazole analogues.

Benzoselenazolium-based hemicyanine dye for G-Quadruplex detection.

Benzothiazolium and benzoxazolium are common groups for the construction of hemicyanine dyes; however, their isosteric analogue benzoselenazolium have rarely been studied. Here, we report the development of the first benzoselenazolium-based hemicyanine dye for the selective detection of G-quadruplexes. This molecule, SEMA-1, was validated as a red-emitting and activatable fluorescent probe whose fluorescence would only be activated in the presence of G-quadruplexes in buffer solution.