Hydrogen peroxide is the most stable reactive oxygen species generated endogenously, participating in numerous physiological processes and abnormal pathological conditions. Mounting evidence suggests that a higher level of H O exists in various disease conditions. Thus, H O functions as an ideal target for site-specific bioimaging and therapeutic targeting. The unique reactivity of organoborons with H O provides a method for developing chemoselective molecules for biological and biomedical applications. This review highlights the design and application of boron-derived molecules for H O detection, and the utility of boron moieties toward masking reactive compounds leading to the development of metal prochelators and prodrugs for selectively delivering an active species at the target sites with elevated H O levels. Additionally, the emergence of H O -responsive theranostic agents consisting of both therapeutic and diagnostic moieties in one integrated system are discussed. The purpose of this review is to provide a better understanding of the role of boron-derived molecules toward biological and pharmacological applications.

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http://dx.doi.org/10.1002/cbic.202100366DOI Listing

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