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

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2021年 / 143卷 / 03期

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

页码：1278 / 1283

页数：6

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