Bisboronic Ester-Enabled Redox-Targeted Cancer Therapy: A Cascade ROS Consumption Approach for Efficient Elimination...

Elevated levels of reactive oxygen species (ROS) in cancer cells, arising from their altered metabolism, represent a distinctive therapeutic target. Here, we introduce the first example of bisboronic esters as potent agents for rapidly disrupting redox homeostasis, selectively inducing oxidative stress to eliminate cancer cells. Structure-activity relationship studies revealed that both the electronic and steric factors significantly influence their cytotoxicity, with the most effective compounds achieving IC₅₀ values as low as 0.63 μM. Confocal imaging confirmed the rapid intracellular depletion of ROS, leading to a severe metabolic imbalance and efficient cancer cell death. This study highlights the potential of boronate-based therapeutics for redox-targeted cancer therapy, which may provide a promising foundation for the development of innovative anticancer strategies.