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Title: Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89

Abstract

The development of bifunctional chelators (BFCs) which can stably chelate zirconium-89 ((89)Zr) while being conjugated to targeting molecules is an area of active research. Herein we report the first octadentate terephthalamide ligands, which are easily radiolabeled with (89)Zr and are highly stable in vitro. Lastly, they represent a novel class of chelators, which are worthy of further development as BFCs for (89)Zr.

Authors:
 [1];  [2];  [3];  [2];  [1]
  1. Wake Forest, Winston-Salem, NC (United States). School of Medicine
  2. Lumiphore, Inc., Berkeley, CA (United States)
  3. Univ. of California, Berkeley, CA (United States). Dept. of Chemistry
Publication Date:
Research Org.:
Washington Univ., St. Louis, MO (United States). School of Medicine
Sponsoring Org.:
USDOE Office of Science (SC), Nuclear Physics (NP)
OSTI Identifier:
1347094
Grant/Contract Number:  
SC0008657; IIP-1215462
Resource Type:
Accepted Manuscript
Journal Name:
ChemComm
Additional Journal Information:
Journal Volume: 51; Journal Issue: 12; Journal ID: ISSN 1359-7345
Publisher:
Royal Society of Chemistry
Country of Publication:
United States
Language:
English
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY

Citation Formats

Pandya, Darpan N., Pailloux, Sylvie, Tatum, David, Magda, Darren, and Wadas, Thaddeus J. Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89. United States: N. p., 2014. Web. doi:10.1039/c4cc09256b.
Pandya, Darpan N., Pailloux, Sylvie, Tatum, David, Magda, Darren, & Wadas, Thaddeus J. Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89. United States. https://doi.org/10.1039/c4cc09256b
Pandya, Darpan N., Pailloux, Sylvie, Tatum, David, Magda, Darren, and Wadas, Thaddeus J. Thu . "Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89". United States. https://doi.org/10.1039/c4cc09256b. https://www.osti.gov/servlets/purl/1347094.
@article{osti_1347094,
title = {Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89},
author = {Pandya, Darpan N. and Pailloux, Sylvie and Tatum, David and Magda, Darren and Wadas, Thaddeus J.},
abstractNote = {The development of bifunctional chelators (BFCs) which can stably chelate zirconium-89 ((89)Zr) while being conjugated to targeting molecules is an area of active research. Herein we report the first octadentate terephthalamide ligands, which are easily radiolabeled with (89)Zr and are highly stable in vitro. Lastly, they represent a novel class of chelators, which are worthy of further development as BFCs for (89)Zr.},
doi = {10.1039/c4cc09256b},
journal = {ChemComm},
number = 12,
volume = 51,
place = {United States},
year = {Thu Dec 18 00:00:00 EST 2014},
month = {Thu Dec 18 00:00:00 EST 2014}
}

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Works referencing / citing this record:

Direct comparison of the in vitro and in vivo stability of DFO, DFO* and DFOcyclo* for 89Zr-immunoPET
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The study of Zr adsorption on nanodispersed hydroxyapatite: X-ray photoelectron study
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A comprehensively revised strategy that improves the specific activity and long-term stability of clinically relevant 89 Zr-immuno-PET agents
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Rational Design, Synthesis and Preliminary Evaluation of Novel Fusarinine C-Based Chelators for Radiolabeling with Zirconium-89
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Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development
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Recent Advances in Zirconium-89 Chelator Development
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