Effect of the type of N-substituent in the benzo-18-azacrown-6 compound on copper(<scp>ii</scp>) chelation: complexation, radiolabeling, stability in vitro, and biodistribution in vivo

Zamurueva, Lyubov S.; Egorova, Bayirta V.; Ikonnikova, I. A.; Zubenko, Anastasia D.; Pashanova, Anna V.; Карноухова, Валентина А.; Mitrofanov, Artem; Trigub, Alexander L.; Moiseeva, Anna A.; Priselkova, Anna B.; Федорова, О. А.; Kalmykov, Stepan N.

doi:10.1039/d3dt00742a

Dalton Trans.

2023

DOI: 10.1039/d3dt00742a

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Effect of the type of N-substituent in the benzo-18-azacrown-6 compound on copper(ii) chelation: complexation, radiolabeling, stability in vitro, and biodistribution in vivo

Lyubov S. Zamurueva

Bayirta V. Egorova

I. A. Ikonnikova

et al.

Abstract: In this work, we synthesized two new benzo-18-azacrown-6 ethers bearing picolinate and pyridine pendant arms and studied the copper complexes of these ligands, as well as those of an acetate...

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2024

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Double-Armed 18- and 21-Membered Macrocycles as Potential Chelators for Lead and Bismuth Radiopharmaceuticals

Zubenko,

Pashanova,

Mosaleva

et al. 2024

Inorg. Chem.

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With increasing clinical applications and interest in targeted alpha therapy, there is growing interest in developing alternative chelating agents for [ 212 Pb]Pb 2+ and [ 212/213 Bi]Bi 3+ that exhibit rapid radiolabeling kinetics and kinetic inertness. Herein we report the synthesis and detailed investigation of diacetate and dipicolinate 18-and 21-membered macrocyclic chelators BADA-18, BADA-21, BADPA-18, and BADPA-21 for the complexation of Pb 2+ and Bi 3+ ions with potential use in the preparation of radiopharmaceuticals. The formation of mononuclear complexes was established by using ESI-mass spectrometry, and their stability constants were determined by potentiometric titration. A thorough study of the structure of the metal complexes was carried out by using X-ray diffraction and NMR spectroscopy. It was shown how the stability of the complex is influenced by an increase in the size of the macrocycle, the replacement of acetate arms with picolinate ones, the rigidity of the ligand, as well as the type of conformation (synor anti-) of the metal complex. The new ligands were radiolabeled with [ 210 Pb]Pb 2+ and [ 207 Bi]Bi 3+ , and the in vitro stability of the resulting complexes in a competitive environment of serum and biologically significant metal ions was assessed. Rapid complex formation in 1−2 min at room temperature, as well as the high kinetic inertness of the complexes Pb(BADPA-18) and Bi(BADPA-18) in biological media, demonstrate its potential for use in targeted radionuclide therapy.

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Double-Armed 18- and 21-Membered Macrocycles as Potential Chelators for Lead and Bismuth Radiopharmaceuticals

Zubenko,

Pashanova,

Mosaleva

et al. 2024

Inorg. Chem.

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show abstract

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Effect of the type of N-substituent in the benzo-18-azacrown-6 compound on copper(ii) chelation: complexation, radiolabeling, stability in vitro, and biodistribution in vivo

Abstract: In this work, we synthesized two new benzo-18-azacrown-6 ethers bearing picolinate and pyridine pendant arms and studied the copper complexes of these ligands, as well as those of an acetate...

Cited by 1 publication

References 59 publications

Double-Armed 18- and 21-Membered Macrocycles as Potential Chelators for Lead and Bismuth Radiopharmaceuticals

Double-Armed 18- and 21-Membered Macrocycles as Potential Chelators for Lead and Bismuth Radiopharmaceuticals

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