Synthesis,64Cu-labeling and PET imaging of 1,4,7-triazacyclononane derived chelators with pendant azaheterocyclic arms
| Autor: | Carla Gotzmann, Friederike Braun, Mark Bartholomä |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
010405 organic chemistry
Reaction step Chemistry Stereochemistry General Chemical Engineering chemistry.chemical_element General Chemistry Pet imaging 010402 general chemistry 01 natural sciences Combinatorial chemistry Copper In vitro 0104 chemical sciences chemistry.chemical_compound In vivo Bifunctional Single crystal Coordination geometry |
| Zdroj: | RSC Advances. 6:119-131 |
| ISSN: | 2046-2069 |
| DOI: | 10.1039/c5ra21131j |
| Popis: | The TACN derived chelators NOTI, NOTI-Me and NOTThia were synthesized in a facile, single reaction step. The new chelators were readily labeled with 64Cu under mild conditions over a wide pH range. The corresponding 64Cu complexes are of high stability in vitro as determined by Cu2+ exchange experiments, acid decomplexation and serum stability studies. Single crystal X-ray analysis showed that the six-coordinate copper complexes exhibited a distorted prismatic CuN3N′3 coordination geometry similar to Cu(NOTA). Biological testing by small animal PET imaging revealed retention of 64Cu complexes in the kidneys and, to a lesser extent, in the liver. Altogether, the results presented support the development of bifunctional derivatives for conjugation to targeting vectors and further testing in vivo. |
| Databáze: | OpenAIRE |
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