2022
DOI: 10.1021/acs.inorgchem.1c03972
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Stable Chelation of the Uranyl Ion by Acyclic Hexadentate Ligands: Potential Applications for 230U Targeted α-Therapy

Abstract: Uranium-230 is an α-emitting radionuclide with favorable properties for use in targeted α-therapy (TAT), a type of nuclear medicine that harnesses α particles to eradicate cancer cells. To successfully implement this radionuclide for TAT, a bifunctional chelator that can stably bind uranium in vivo is required. To address this need, we investigated the acyclic ligands H 2 dedpa, H 2 CHXdedpa, H 2 hox, and H 2 CHXhox as uranium chelators. The stability constants of these ligands with UO 2 2+ were measured via s… Show more

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Cited by 13 publications
(7 citation statements)
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“…The stability constants determined for the Ln 3+ complexes of CHX OCTAPA 4– by different methods (pH-potentiometry and 1 H-relaxometry) are in excellent agreement, being comparable with those reported for the analogues with OCTAPA 4– (Table ). , This indicates that the replacement of the ethylenediamine spacer by a more rigid cyclohexyl group does not have a significant impact on complex stability, as observed recently for uranyl complexes . The stability constants characterizing the Ln 3+ complexes of CHX OCTAPA 4– are similar to those of DO3A 3– , , but remain lower than those reported for the analogous DOTA 4– complexes. , We note that the stability constants determined in 0.1 M KCl and 0.15 M NaCl for the Gd 3+ complex of DTPA 5– are in good agreement, while there is a significant difference in the case of DO3A 3– .…”
Section: Resultssupporting
confidence: 79%
“…The stability constants determined for the Ln 3+ complexes of CHX OCTAPA 4– by different methods (pH-potentiometry and 1 H-relaxometry) are in excellent agreement, being comparable with those reported for the analogues with OCTAPA 4– (Table ). , This indicates that the replacement of the ethylenediamine spacer by a more rigid cyclohexyl group does not have a significant impact on complex stability, as observed recently for uranyl complexes . The stability constants characterizing the Ln 3+ complexes of CHX OCTAPA 4– are similar to those of DO3A 3– , , but remain lower than those reported for the analogous DOTA 4– complexes. , We note that the stability constants determined in 0.1 M KCl and 0.15 M NaCl for the Gd 3+ complex of DTPA 5– are in good agreement, while there is a significant difference in the case of DO3A 3– .…”
Section: Resultssupporting
confidence: 79%
“…The 8-hydroxyquinoline-2-carbaldehyde 3 and 2-chloroquinolin-8-ol 4 were prepared according to the method described in the literature [ 26 , 42 ].…”
Section: Methodsmentioning
confidence: 99%
“…Evidently, while UO 2 2+ coordination chemistry in anhydrous solvents has been subject to long-standing interest in the f-element community, stabilization of chelation in biological media is to date widely lacking yet an attractive emerging challenge with importance for nuclear medicine applications. 4 Another significant challenge for the development of f-elements as radiopharmaceuticals is the lack of available diagnostic congeners. Small ions with PET isotopes, such as Sc 3+ , Y 3+ and Zr 4+ cannot accurately capture the chemical behavior, and as a result, biological properties of the large triand tetravalent f-elements.…”
Section: Current Challenges and Opportunitiesmentioning
confidence: 99%
“…Evidently, while UO 2 2+ coordination chemistry in anhydrous solvents has been subject to long-standing interest in the f-element community, stabilization of chelation in biological media is to date widely lacking yet an attractive emerging challenge with importance for nuclear medicine applications. 4…”
Section: Radiometals In Diagnostic and Therapeutic Nuclear Medicinementioning
confidence: 99%