| Full text | |
| Author(s): |
Prado, Viviana S.
[1]
;
Leitao, Renan C. F.
[1]
;
Silva, Francisco
[2]
;
Gano, Lurdes
[2]
;
Santos, Isabel C.
[2]
;
Marques, Fabio L. N.
[3]
;
Paulo, Antonio
[2]
;
Deflon, Victor M.
[1]
Total Authors: 8
|
| Affiliation: | [1] Univ Sao Paulo, Inst Quim Sao Carlos, BR-13566590 Sao Carlos, SP - Brazil
[2] Univ Lisbon, Inst Super Tecn, Ctr Ciencias & Tecnol Nucl, Estr Nacl 10, P-2695066 Bobadela Lrs - Portugal
[3] Univ Sao Paulo, Fac Med, Dept Radiol & Oncol, Lab Med Nucl LIM 43, BR-05403911 Sao Paulo, SP - Brazil
Total Affiliations: 3
|
| Document type: | Journal article |
| Source: | DALTON TRANSACTIONS; v. 50, n. 5 FEB 7 2021. |
| Web of Science Citations: | 0 |
| Abstract | |
The synthesis of two new hexadentate potentially tetra-anionic acyclic chelators, an N2O4-donor bis(semicarbazone) (H(4)bsc) and an N2O2S2-donor bis(thiosemicarbazone) (H(4)btsc), is described. Coordination reactions of the ligands with gallium and indium precursors were investigated and yielded the complexes {[}Ga(Hbsc)] (1) and {[}In(Hbtsc)] (2), respectively. Ligands and complexes structures were confirmed by several techniques, including FTIR, NMR (H-1, C-13, COSY, HSQC), ESI(+)-MS and single crystal X-ray diffraction analysis. The radioactive congeners {[}Ga-67(Hbsc)] (1{*}) and {[}In-111(Hbtsc)] (2{*}) were also synthesized and their radiolabeling yield and radiochemical purity were certified by HPLC and ITLC analyses. Biodistribution assays in groups of CD-1 mice showed a high uptake of both radiocomplexes in liver and intestine where 1{*} presented higher retention. In vitro and in vivo assays revealed higher stability of 1{*} compared with 2{*}, namely in the blood. The results suggest that radiocomplex 1{*} is a candidate for further investigation as it could be prepared in high yields (>95%), at low temperature (20-25 degrees C) and at fast reaction time (15 min), which are very desirable synthesis conditions for potential new radiopharmaceuticals. (AU) | |
| FAPESP's process: | 09/54011-8 - Acquisition of a single-crystal X-ray diffractometer for the structural analysis of small molecules and proteins |
| Grantee: | Victor Marcelo Deflon |
| Support Opportunities: | Multi-user Equipment Program |
| FAPESP's process: | 09/54040-8 - Acquisition of a high-resolution Orbitrap mass spectrometer for the discovery and structural analysis of biologically active compounds: applications in proteomics, biomarkers, synthesis, isolation, and characterization of natural products, studies of redox systems in food and enzymatic synthesis |
| Grantee: | Emanuel Carrilho |
| Support Opportunities: | Multi-user Equipment Program |