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Deferasirox (ExJade): An FDA-Approved AIEgen Platform with Unique Photophysical Properties
Journal of the American Chemical Society ( IF 14.4 ) Pub Date : 2021-01-11 , DOI: 10.1021/jacs.0c11641
Adam C Sedgwick 1 , Kai-Cheng Yan 2 , Daniel N Mangel 1 , Ying Shang 2 , Axel Steinbrueck 1 , Hai-Hao Han 2 , James T Brewster 1 , Xi-Le Hu 2 , Dylan W Snelson 1 , Vincent M Lynch 1 , He Tian 2 , Xiao-Peng He 2 , Jonathan L Sessler 1
Affiliation  

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.

中文翻译:

Deferasirox (ExJade):FDA 批准的具有独特光物理特性的 AIEgen 平台

Deferasirox (ExJade) 是 FDA 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,它们显示出独特的光物理特性,即聚集诱导发射 (AIE)、激发态分子内质子转移、电荷转移以及水介质中的键合和空间共轭特性。地拉罗司支架上苯酚单元的功能化提供了荧光响应前螯合剂 ExPhos,它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。
更新日期:2021-01-11
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