New bioconjugated technetium and rhenium folates synthesized by transmetallation reaction with zinc derivatives
Borràs, Jordi (Universitat Autònoma de Barcelona. Departament de Química)
Foster, Julie ![Identificador ORCID](/img/uab/orcid.ico)
(Queen Mary University of London)
Kashani, Roxana (Queen Mary University of London)
Melendez-Alafort, L. ![Identificador ORCID](/img/uab/orcid.ico)
(Istituto Oncologico Veneto IRCCS)
Sosabowski, Jane ![Identificador ORCID](/img/uab/orcid.ico)
(Queen Mary University of London)
Suades Ortuño, Joan ![Identificador ORCID](/img/uab/orcid.ico)
(Universitat Autònoma de Barcelona. Departament de Química)
Barnadas Rodríguez, Ramon
(Universitat Autònoma de Barcelona. Departament de Bioquímica i de Biologia Molecular)
Fecha: |
2021 |
Resumen: |
The zinc dithiocarbamates functionalized with folic acid 2 and 3 were synthesized with a simple straightforward method, using an appropriated folic acid derivative and a functionalized zinc dithiocarbamate (1). Zinc complexes 2 and 3 show very low solubilities in water, making them useful for preparing Tc-99m radiopharmaceuticals with a potentially high molar activity. Thus, the transmetallation reaction in water medium between the zinc complexes 2 or 3 and the cation fac-[ Tc(H O) (CO) ], in the presence of the monodentate ligand TPPTS, leads to the formation of the 2 + 1 complexes fac-[ Tc(CO) (SS)(P)] bioconjugated to folic acid (2 and 3). In spite of the low solubility of 2 and 3 in water, the reaction yield is higher than 95%, and the excess zinc reagent is easily removed by centrifugation. The Tc-99m complexes were characterized by comparing their HPLC with those of the homologous rhenium complexes (2 and 3) previously synthesized and characterized by standard methods. Preliminary in vivo studies with 2 and 3 indicate low specific binding to folate receptors. In summary, Tc-99m folates 2 and 3 were prepared in high yields, using a one-pot transmetallation reaction with low soluble zinc dithiocarbamates (>1 ppm), at moderate temperature, without needing a subsequent purification step. |
Ayudas: |
Ministerio de Economía y Competitividad BIO2015-67358-C2-2-P Ministerio de Economía y Competitividad CTQ2015-70371-REDT Agència de Gestió d'Ajuts Universitaris i de Recerca 2017/SGR-795
|
Derechos: |
Aquest document està subjecte a una llicència d'ús Creative Commons. Es permet la reproducció total o parcial, la distribució, la comunicació pública de l'obra i la creació d'obres derivades, fins i tot amb finalitats comercials, sempre i quan es reconegui l'autoria de l'obra original. ![Creative Commons](/img/licenses/by.ico) |
Lengua: |
Anglès |
Documento: |
Article ; recerca ; Versió publicada |
Materia: |
Technetium ;
Carbonyl ;
Folic ;
Transmetallation ;
Radiopharmaceutical ;
Rhenium |
Publicado en: |
Molecules, Vol. 26, Núm. 8 (April 2021) , art. 2373, ISSN 1420-3049 |
DOI: 10.3390/molecules26082373
PMID: 33921789
El registro aparece en las colecciones:
Artículos >
Artículos de investigaciónArtículos >
Artículos publicados
Registro creado el 2021-12-20, última modificación el 2022-07-30