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辐射响应型苯并噻唑啉作为潜在的可切割荧光连接物用于药物传递。

Radiation-Responsive Benzothiazolines as Potential Cleavable Fluorogenic Linkers for Drug Delivery.

机构信息

CEA, INRAE, Département Médicaments et Technologies pour la Santé (DMTS), SCBM, Université Paris Saclay, 91191, Gif-sur-Yvette, France.

LIONS, NIMBE, CEA, CNRS, Université Paris-Saclay, 91191, Gif-sur-Yvette, France.

出版信息

Chemistry. 2023 Jun 2;29(31):e202300358. doi: 10.1002/chem.202300358. Epub 2023 Apr 24.

Abstract

Radiosensitive compounds can be useful for the detection of radiations and also as prodrugs that can be activated during a radiotherapy. Herein we describe the use of benzothiazolines, which upon treatment with Cs produced γ-irradiation in water give rise to fluorescent benzothiazoles and concomitant release of amines or carboxylic acids. In a proof of concept study, we showed that benzothiazolines may be used as new cleavable linkers that can be triggered upon irradiation.

摘要

辐射敏感化合物可用于辐射检测,也可用作前药,在放射治疗过程中被激活。本文描述了苯并噻唑啉的应用,用 Cs 处理后,在水中产生 γ 射线辐照,生成荧光苯并噻唑,并同时释放胺或羧酸。在概念验证研究中,我们表明苯并噻唑啉可用作新的可裂解连接物,可在辐照时触发。

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