Bisindole-based small molecules as transmembrane anion transporters and potential anticancer agents

Few synthetic ion transporters have been reported incorporating indole as the core moiety. We have developed a novel bisindole-based transporter capable of efficient transmembrane anion antiport. This system induced cytotoxicity in MCF-7 breast cancer cells via chloride ion homeostasis disruption and the associated ROS generation, mitochondrial membrane depolarization, and lysosomal deacidification. A bisindole-based transmembrane anion antiporter, selectively toxic to the MCF-7 cancer cells, where chloride transport-induced homeostasis disruption triggered mitochondrial membrane depolarization, ROS generation, and lysosomal deacidification.