4.8 Article

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

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 143, Issue 3, Pages 1278-1283

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jacs.0c11641

Keywords

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Funding

  1. National Natural Science Foundation of China [21788102, 91853201, 21722801, 81673489, 31871414]
  2. National Science and Technology Major Project of China [2018ZX10732202]
  3. Shanghai Municipal Science and Technology Major Project [2018SHZDZX03]
  4. International Cooperation Program of Shanghai Science and Technology Committee [17520750100]
  5. Fundamental Research Funds for the Central Universities [222201717003]
  6. National Institutes of Health [R01 GM103790]
  7. Robert A. Welch Foundation [F-0018]

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In this study, fluorescent deferasirox derivatives with unique photophysical properties were reported, and a fluorescent responsive pro-chelator was successfully developed for the detection of alkaline phosphatase. The diagnostic potential of these deferasirox derivatives in bacterial biofilm studies was demonstrated.
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.

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