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Title: Structurally Defined Water‐Soluble Metallofullerene Derivatives towards Biomedical Applications

Journal Article · · Angewandte Chemie (International Edition)
 [1];  [1];  [1];  [2];  [3];  [1];  [1];  [1];  [1];  [4];  [2];  [3];  [3];  [1];  [5]; ORCiD logo [1]
  1. Department of Chemistry and Chemical Biology, Rutgers The State University of New Jersey 123 Bevier Rd Piscataway NJ 08854 USA
  2. National High Magnetic Field Laboratory (NHMFL) Florida State University 1800 E. Paul Dirac Dr. Tallahassee FL 32310 USA
  3. Departament de Química Física i Inorgànica Universitat Rovira i Virgili Marcel⋅lí Domingo 1 43007 Tarragona Spain
  4. Department of Physics and Astronomy, Rutgers The State University of New Jersey 136 Frelinghuysen Rd Piscataway NJ 08854 USA
  5. National High Magnetic Field Laboratory (NHMFL) Florida State University 1800 E. Paul Dirac Dr. Tallahassee FL 32310 USA, Department of Physics Florida State University Tallahassee FL 32306 USA

Abstract Endohedral metallofullerenes (EMFs) are excellent carriers of rare‐earth element (REE) ions in biomedical applications because they preclude the release of toxic metal ions. However, existing approaches to synthesize water‐soluble EMF derivatives yield mixtures that inhibit precise drug design. Here we report the synthesis of metallobuckytrio (MBT), a three‐buckyball system, as a modular platform to develop structurally defined water‐soluble EMF derivatives with ligands by choice. Demonstrated with PEG ligands, the resulting water‐soluble MBTs show superb biocompatibility. The Gd MBTs exhibit superior T 1 relaxivity than typical Gd complexes, potentially superseding current clinical MRI contrast agents in both safety and efficiency. The Lu MBTs generated reactive oxygen species upon light irradiation, showing promise as photosensitizers. With their modular nature to incorporate other ligands, we anticipate the MBT platform to open new paths towards bio‐specific REE drugs.

Research Organization:
Florida State University, Tallahassee, FL (United States)
Sponsoring Organization:
National Institutes of Health (NIH); National Science Foundation (NSF); Spanish Ministry of Science and Innovation; USDOE; USDOE Office of Science (SC)
Grant/Contract Number:
SC0020260
OSTI ID:
1902485
Journal Information:
Angewandte Chemie (International Edition), Journal Name: Angewandte Chemie (International Edition) Journal Issue: 3 Vol. 62; ISSN 1433-7851
Publisher:
Wiley Blackwell (John Wiley & Sons)Copyright Statement
Country of Publication:
Germany
Language:
English

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