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DOI: 10.1055/s-0039-1691540
Synthetic Approaches to the Bifunctional Chelators for Radionuclides Based On Pyridine-Containing Azacrown Compounds
The work was supported by Russian Science Foundation (grant No 16-13-10226). The characterization of the products was performed with the financial support from the Ministry of Science and Higher Education of the Russian Federation using the equipment of Center for molecular composition studies of INEOS RAS.Publikationsverlauf
Received: 11. Oktober 2019
Accepted after revision: 03. Dezember 2019
Publikationsdatum:
16. Dezember 2019 (online)


Abstract
Synthetic ways to introduce functional groups (CO2Me, CO2H, OCH2CO2H, OCH2C≡CH, CH2OH, CH2Cl, CH2N3) into the pyridine ring of pyridine-containing azacrown compounds are described. These groups were introduced at position-4 of the pyridine ring, while keeping the macrocyclic carboxylate groups available for metal chelation. The derivatives were obtained by macrocyclization reaction of 4-substituted, trimethyl pyridine-2,4,6-tricarboxylate or by modification of methyl ester group in pyridine fragment of macrocycles. Obtained derivatives can be applied for preparing radiotherapeutic agents by conjugation to different vector biomolecules for targeted drug delivery to cancer cells without damaging healthy tissue.
Key words
bifunctional chelators - azacrown compounds - macrocyclization - radiopharmaceuticals - bioconjugationSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0039-1691540.
- Supporting Information