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地拉罗司(Exjade):具有独特光物理特性的美国 FDA 批准的聚集诱导发光剂平台。

Deferasirox (ExJade): An FDA-Approved AIEgen Platform with Unique Photophysical Properties.

机构信息

Department of Chemistry, The University of Texas at Austin, 105 East 24th Street-A5300, Austin, Texas 78712-1224, United States.

Key Laboratory for Advanced Materials and Joint International Research Laboratory of Precision Chemistry and Molecular Engineering, Feringa Nobel Prize Scientist Joint Research Center, Frontiers Center for Materiobiology and Dynamic Chemistry, School of Chemistry and Molecular Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.

出版信息

J Am Chem Soc. 2021 Jan 27;143(3):1278-1283. doi: 10.1021/jacs.0c11641. Epub 2021 Jan 11.

Abstract

Deferasirox, ExJade, is an FDA-approved iron chelator used for the treatment of iron overload. In this work, we report several fluorescent deferasirox derivatives that display unique photophysical properties, i.e., aggregation-induced emission (AIE), excited state intramolecular proton transfer, charge transfer, and through-bond and through-space conjugation characteristics in aqueous media. Functionalization of the phenol units on the deferasirox scaffold afforded the fluorescent responsive pro-chelator ExPhos, which enabled the detection of the disease-based biomarker alkaline phosphatase (ALP). The diagnostic potential of these deferasirox derivatives was supported by bacterial biofilm studies.

摘要

地拉罗司,ExJade,是一种获得美国食品药品监督管理局批准的铁螯合剂,用于治疗铁过载。在这项工作中,我们报告了几种荧光地拉罗司衍生物,它们在水介质中表现出独特的光物理性质,即聚集诱导发射(AIE)、激发态分子内质子转移、电荷转移以及通过键和离域共轭特性。地拉罗司骨架上的酚单元的功能化得到了荧光响应前螯合剂 ExPhos,这使得能够检测基于疾病的生物标志物碱性磷酸酶(ALP)。这些地拉罗司衍生物的诊断潜力得到了细菌生物膜研究的支持。

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