4.8 Article

A Macrocyclic Chelator with Unprecedented Th4+ Affinity

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JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 136, 期 25, 页码 9106-9115

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AMER CHEMICAL SOC
DOI: 10.1021/ja503456r

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  1. Division of Chemical Sciences, Geosciences, and Biosciences of the U.S. Department of Energy at LBNL [DE-AC02-05CH11231]
  2. NSF [CHE-0840505]

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A novel macrocyclic octadentate ligand incorporating terephthalamide binding units has been synthesized and evaluated for the chelation of Th4+. The thorium complex was structurally characterized by X-ray diffraction and in solution with kinetic studies and spectrophotometric titrations. Dye displacement kinetic studies show that the ligand is a, much more rapid chelator of Th4+ than prevailing ligands (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid and diethylenetriaminepentaacetic acid). Furthermore, the resulting complex was found to have a remarkably high thermodynamic stability, with a formation constant of 10(54). These data support potential radiotherapeutic applications.

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