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

被引:56
作者
Sedgwick, Adam C. [1 ]
Yan, Kai-Cheng [2 ,3 ]
Mangel, Daniel N. [1 ]
Shang, Ying [2 ,3 ]
Steinbrueck, Axel [1 ]
Han, Hai-Hao [2 ,3 ]
Brewster, James T., II [1 ]
Hu, Xi-Le [2 ,3 ]
Snelson, Dylan W. [1 ]
Lynch, Vincent M. [1 ]
Tian, He [2 ,3 ]
He, Xiao-Peng [2 ,3 ]
Sessler, Jonathan L. [1 ]
机构
[1] Univ Texas Austin, Dept Chem, Austin, TX 78712 USA
[2] East China Univ Sci & Technol, Feringa Nobel Prize Scientist Joint Res Ctr, Key Lab Adv Mat, Sch Chem & Mol Engn,Frontiers Ctr Materiobiol & D, Shanghai 200237, Peoples R China
[3] East China Univ Sci & Technol, Feringa Nobel Prize Scientist Joint Res Ctr, Joint Int Res Lab Precis Chem & Mol Engn, Sch Chem & Mol Engn,Frontiers Ctr Materiobiol & D, Shanghai 200237, Peoples R China
基金
美国国家卫生研究院; 中国国家自然科学基金;
关键词
Chelation - Diagnosis - Fluorescence - Iron - Charge transfer - Scaffolds (biology) - Scaffolds - Phosphatases;
D O I
10.1021/jacs.0c11641
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
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.
引用
收藏
页码:1278 / 1283
页数:6
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