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Radiation-Responsive Benzothiazolines as Potential Cleavable Fluorogenic Linkers for Drug Delivery
Wei Tuo1, Jean-Philippe Renault2, Aashini Rajpal2
1CEA, INRAE, Département Médicaments et Technologies pour la Santé (DMTS), SCBM, Université Paris Saclay, 91191, Gif-sur-Yvette, France.
Chemistry (Weinheim an Der Bergstrasse, Germany)
|March 28, 2023
Summary
New benzothiazoline compounds become fluorescent and release molecules when exposed to radiation. This discovery offers potential for radiation detection and targeted drug delivery in radiotherapy, utilizing radiation-triggered cleavable linkers.
Area of Science:
- * Radiochemistry and Materials Science: Investigating the development of novel radiosensitive compounds.
Background:
- * Radiosensitive compounds offer dual utility in radiation detection and as targeted prodrugs activated during radiotherapy.
- * Benzothiazolines are a class of compounds with potential radiosensitive properties.
Purpose of the Study:
- * To explore the radiosensitive properties of benzothiazolines.
- * To demonstrate their utility as radiation-triggered cleavable linkers.
Main Methods:
- * Treatment of benzothiazolines with 137Cs gamma irradiation in aqueous solution.
- * Observation of fluorescence generation and amine/carboxylic acid release.
Main Results:
- * Benzothiazolines were converted to fluorescent benzothiazoles upon gamma irradiation.
- * Concomitant release of amines or carboxylic acids was observed, indicating linker cleavage.
- * Proof-of-concept study confirmed benzothiazolines as effective radiation-triggered cleavable linkers.
Conclusions:
- * Benzothiazolines exhibit radiosensitivity, producing fluorescence and releasing molecules upon irradiation.
- * These compounds represent a novel class of cleavable linkers activated by radiation.
- * Potential applications include radiation detection and targeted prodrug activation in radiotherapy.
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