Publications Repository - Helmholtz-Zentrum Dresden-Rossendorf

2 Publications
Sulfonated calix-baskets for complexation of Barium and Radium
Mamat, C.ORC; Reissig, F.ORC; Bauer, D.ORC; Pietzsch, H.-J.ORC; Steinbach, J.ORC
Understanding the coordination chemistry of heavy group 2 metals, especially of barium as surrogate for radium, is mandatory not only for radiopharmaceutical applications of radium. This is from high importance since radium-223 is the only approved therapeutic alpha-emitter (by EMA and FDA). Unfortunately, the applications are limited. To date, radium-223 is only in use as RaCl2 for the treatment of bone cancer metastases. To overcome this limitation, which is also true for other group 2 metals, special cage-like compounds have to be developed as ligands like sulfonated calix[4]crowns to stably bind the Ba2+ and Ra2+ to avoid a release in vivo. This will be the basis for a future application of heavy group 2 metals and not only of radium to treat other cancer entities than bone metastases. Ra2+ can then be included in radiopharmaceuticals which contain a chelator and a biologically active molecule part to find the tumor cell.
For this purpose, a series of modified calix[4]crown-6 derivatives was synthesized to chelate barium, which serves as non-radioactive surrogate for radium-223/-224. These calixcrowns were functionalized sulfonate moieties including deprotonable groups and the corresponding barium complexes were synthesized. Stability constants of these complexes were measured using UV/Vis titration experiments to determine logK values. Further extraction studies were performed with [133Ba]Ba2+ and [224Ra]Ra2+ to further characterize the binding affinity of calixcrowns.
  • Lecture (Conference)
    RadChem - 18th Radiochemical Conference, 13.-18.05.2018, Mariánské Lázně, Czech Republic
  • Open Access LogoContribution to proceedings
    RadChem - 18th Radiochemical Conference, 13.-18.05.2018, Mariánské Lázne, Czech Republic
    Czech Chemical Society Symposium Series, Praha: Czech Chemical Society (CCS), 228-229

Publ.-Id: 27462 - Permalink