Synthesis and mechanism study of a new bi-gold compound targeting mitochondria to eliminate cancer stem cells

Our work demonstrate that the increase of positive charge could generally gain anticancer potency for gold-containing compounds. The bi-gold series compounds (series 2) generally exhibited better potency to inhibit cancer cells. The best compound BGC2a was accumulated preferentially within mitochondria, leading to increase of ROS and disruption of mitochondrial function. BGC2a was more effective in lung cancer cells with high stem-like side population and glioblastoma stem cells. In-vivo animal study confirmed that BGC2a effectively suppressed tumor growth of lung cancer xenograft, which is also validated in the pancreatic cancer xenograft model.
The raw data associated with the figures in manuscript are contained. Of note, some of them are in .pzfx format that can be viewed by GraphPad software (V6 and above). NMR spectra of the synthetic compounds are in .mnova format that can be viewed by MestReNova software.