Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms: Toward New Pharmaceuticals for β-Radiotherapy

Mariane Le Fur, Maryline Beyler, Eniko Molnár, Olivier Fougère, David Esteban-Gómez, G. Tircsó, Carlos Platas-Iglesias, Nicolas Lepareur, Olivier Rousseaux, Raphaël Tripier

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

We report the synthesis of two azaligands based on the pyclen macrocyclic platform containing two picolinate and one acetate pendant arms. The two ligands differ in the relative positions of the pendant functions, which are arranged either in a symmetrical (L3) or nonsymmetrical (L4) fashion. The complexation properties of the ligands toward natY3+ and 90Y3+ were investigated to assess their potential as chelating units for radiopharmaceutical applications. The X-ray structures of the YL3 and YL4 complexes show nonadentate binding of the ligand to the metal ions. A multinuclear 1H, 13C, and 89Y NMR study shows that the complexes present a structure in solution similar to that observed in the solid state. The two complexes present very high thermodynamic stability constants (log KYL = 23.36(2) and 23.07(2) for YL3 and YL4, respectively). The complexes also show a remarkable inertness with respect to their proton-assisted dissociation, especially YL4. 90Y radiolabeling was proved to be efficient under mild conditions. The 90YL3 and 90YL4 radiochelates were found to be more stable than 90Y(DOTA).

Original languageEnglish
Pages (from-to)2051-2063
Number of pages13
JournalInorganic Chemistry
Volume57
Issue number4
DOIs
Publication statusPublished - Feb 19 2018

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Bearings (structural)
Yttrium
Radiotherapy
yttrium
radiation therapy
Ligands
ligands
Pharmaceutical Preparations
Radiopharmaceuticals
Chelation
Complexation
Metal ions
Protons
acetates
metal ions
Acetates
Thermodynamic stability
platforms
Nuclear magnetic resonance
dissociation

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Inorganic Chemistry

Cite this

Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms : Toward New Pharmaceuticals for β-Radiotherapy. / Le Fur, Mariane; Beyler, Maryline; Molnár, Eniko; Fougère, Olivier; Esteban-Gómez, David; Tircsó, G.; Platas-Iglesias, Carlos; Lepareur, Nicolas; Rousseaux, Olivier; Tripier, Raphaël.

In: Inorganic Chemistry, Vol. 57, No. 4, 19.02.2018, p. 2051-2063.

Research output: Contribution to journalArticle

Le Fur, M, Beyler, M, Molnár, E, Fougère, O, Esteban-Gómez, D, Tircsó, G, Platas-Iglesias, C, Lepareur, N, Rousseaux, O & Tripier, R 2018, 'Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms: Toward New Pharmaceuticals for β-Radiotherapy', Inorganic Chemistry, vol. 57, no. 4, pp. 2051-2063. https://doi.org/10.1021/acs.inorgchem.7b02953
Le Fur, Mariane ; Beyler, Maryline ; Molnár, Eniko ; Fougère, Olivier ; Esteban-Gómez, David ; Tircsó, G. ; Platas-Iglesias, Carlos ; Lepareur, Nicolas ; Rousseaux, Olivier ; Tripier, Raphaël. / Stable and Inert Yttrium(III) Complexes with Pyclen-Based Ligands Bearing Pendant Picolinate Arms : Toward New Pharmaceuticals for β-Radiotherapy. In: Inorganic Chemistry. 2018 ; Vol. 57, No. 4. pp. 2051-2063.
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