Benzoazacrown compound: a highly effective chelator for therapeutic bismuth radioisotopes

Ekaterina V. Matazova; Bayirta V. Egorova; Ekaterina A. Konopkina; Gleb Yu. Aleshin; Anastasia D. Zubenko; Artem A. Mitrofanov; Kirill V. Karpov; Olga A. Fedorova; Yuri V. Fedorov; Stepan N. Kalmykov

doi:10.1039/C9MD00251K

Benzoazacrown compound: a highly effective chelator for therapeutic bismuth radioisotopes†

Ekaterina V. Matazova,

^a Bayirta V. Egorova,

*^a Ekaterina A. Konopkina,^a Gleb Yu. Aleshin,^a Anastasia D. Zubenko,^b Artem A. Mitrofanov,

^ac Kirill V. Karpov,^c Olga A. Fedorova,

^abd Yuri V. Fedorov

^b and Stepan N. Kalmykov^ae

Author affiliations

* Corresponding authors

^a Lomonosov Moscow State University, 119991 Leninskie Gory, 1/3, Moscow, Russian Federation
E-mail: bayirta.egorova@gmail.com

^b A. N. Nesmeyanov Institute of Organoelement Compounds of Russian Academy of Sciences, 119991 Vavilova, 28, GSP-1, Moscow, Russian Federation

^c Science Data Software, Rockville, MD, USA

^d Mendeleev University of Chemistry and Technology of Russia, 125047 Miusskaya sqr., 9, Moscow, Russian Federation

^e National Research Center “Kurchatov Institute”, 123098 Akademika Kurchatova sqr., 1, Moscow, Russian Federation

Abstract

A new benzoazacrown ligand H₄BATA was synthesized and its complexation ability towards bismuth cations was evaluated. Binding of cation occurs at room temperature in a few minutes and formed complex exhibits the same level of inertness as highly stable complex with the well-known H₄DOTA in biologically relevant and challenging media under in vivo conditions.

MedChemComm

Benzoazacrown compound: a highly effective chelator for therapeutic bismuth radioisotopes†

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Benzoazacrown compound: a highly effective chelator for therapeutic bismuth radioisotopes

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