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Thioether Oxidation Chemistry in Reactive Oxygen Species (ROS)-Sensitive Trigger Design: A Kinetic Analysis

A. Abdel‐Fattah, Shubham Bansal, Joanna Afokai Quaye, Shameer M. Kondengadan, Giovanni Gadda, Binghe Wang

2025Organic Letters22 citationsDOIOpen Access PDF

Abstract

High Resolution Image Download MS PowerPoint Slide Thioether oxidation to sulfoxide by H 2 O 2 has been widely reported as an ROS-sensitive trigger in drug delivery applications. Through a number of straightforward kinetic experiments with a series of aryl thioethers, we show that H 2 O 2 oxidation under near-physiological conditions is expected to have half-lives on the scale of hundreds of hours at pathophysiologically relevant H 2 O 2 concentrations. On the other hand, hypochlorite can oxidize thioethers at much faster rates with half-lives in the range of seconds to sulfoxide and minutes to sulfone under similar conditions. Such information means that hypochlorite likely plays a much more important role than H 2 O 2 in activating thioether-based drug delivery systems.

Topics & Concepts

ChemistryThioetherReactive oxygen speciesOxygenKinetic energyCombinatorial chemistryOrganic chemistryBiochemistryPhysicsQuantum mechanicsFree Radicals and AntioxidantsSulfur Compounds in BiologyRedox biology and oxidative stress
Thioether Oxidation Chemistry in Reactive Oxygen Species (ROS)-Sensitive Trigger Design: A Kinetic Analysis | Litcius