Novel [99mTcIII(PS)2(Ln)] Mixed-Ligand Compounds (PS = Phosphino-thiolate; L = Dithiocarbamate) Useful in Design and Development of TcIII-Based Agents: Synthesis, in Vitro, and ex Vivo Biodistribution Studies
| Autor: | Antonio Rosato, Cristina Bolzati, Fiorenzo Refosco, Nicola Salvarese, Nicolò Morellato, Laura Meléndez-Alafort |
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| Rok vydání: | 2014 |
| Předmět: |
Male
Biodistribution IMAGING AGENTS RADIOPHARMACEUTICALS Stereochemistry Ethanethiol Ligands Rats Sprague-Dawley chemistry.chemical_compound Pyrrolidine dithiocarbamate CHEMISTRY Drug Discovery Animals Humans Moiety Tissue Distribution CRYSTAL-STRUCTURE PEPTIDE Chelation Dithiocarbamate Chromatography High Pressure Liquid chemistry.chemical_classification COORDINATION Ligand RHENIUM Technetium Organotechnetium Compounds TC-99M chemistry Molecular Medicine Chemical stability RADIOTRACER TECHNETIUM COMPLEXES |
| Zdroj: | Journal of medicinal chemistry 57 (2014): 8960–8970. doi:10.1021/jm501088w info:cnr-pdr/source/autori:Salvarese N.; Morellato N.; Rosato A.; Melendez-Alafort L.; Refosco F.; Bolzati C./titolo:Novel [Tc-99m(III)(PS)(2)(Ln)] Mixed-Ligand Compounds (PS = Phosphinothiolate; L = Dithiocarbamate) Useful in Design and Development of Tc-III-Based Agents: Synthesis, in Vitro, and ex Vivo Biodistribution Studies/doi:10.1021%2Fjm501088w/rivista:Journal of medicinal chemistry/anno:2014/pagina_da:8960/pagina_a:8970/intervallo_pagine:8960–8970/volume:57 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm501088w |
| Popis: | A general procedure for the preparation of a new class of neutral six-coordinated mixed ligand [Tc-99m(III)(PS)(2)(Ln)] compounds (PS = trisalkyl-phosphino-thiolate; Ln = dithiocarbamate) is reported as well as their in vitro stability and the ex vivo tissue distribution studies. [Tc-99m(PS)(2)(Ln)] complexes were prepared in high yield in nearly physiologic conditions following a one-pot procedure. For instance, the chemical identity of [Tc-99m(PSiso)(2)(L1)] (PSiso = 2-(diisopropylphosphino)ethanethiol; L1 = pyrrolidine dithiocarbamate) was determined by HPLC comparison with the corresponding (99g)Tc-complex. All complexes comprise the stable [Tc-99m(III)(PS)(2)](+) moiety, where the remaining two coordination positions are saturated by a dithiocarbamate chelate, also carrying bioactive molecules (e.g., 2-methoxyphenylpiperazine). [Tc-99m(PS)(2)(Ln)] complexes were inert toward ligand exchange reactions. No significant in vitro and in vivo biotransformation were observed, underlining their remarkable thermodynamic stability and kinetic inertness. These results could be conveniently utilized to devise a novel class of Tc-99m(III)-based compounds useful in radiopharmaceutical applications. |
| Databáze: | OpenAIRE |
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