[natY/90Y]Yttrium and [natLu/177Lu]Lutetium Complexation by Rigid H4OCTAPA Derivatives. Effect of Ligand Topology
2025
Lucio-Martínez, Fátima | Szilagyi, Balazs | Uzal-Varela, Rocío | Perez-Lourido, Paulo | Esteban-Gómez, David | Lepareur, Nicolas | Tircsó, Gyula | Platas-Iglesias, Carlos | Universidade da Coruña | University of Debrecen | Universidade de Vigo | Nutrition, Métabolismes et Cancer (NuMeCan) ; Université de Rennes (UR)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Institut National de Recherche pour l’Agriculture, l’Alimentation et l’Environnement (INRAE) | CRLCC Eugène Marquis (CRLCC) ; UNICANCER | Ministerio de Ciencia e Innovacion; Xunta de Galicia; Hungarian National Research, Development and Innovation Office; University of Debrecen's Publication Support Programme; Doctoral School of Chemistry at the University of Debrecen, Hungary; Labex Iron [ANR-11-LABX-0018]; International Atomic Energy Agency (IAEA) [F22078]; [PID2022-138335NB-I00]; [ED431C 2023/33]; [NKFIH K-134694]. This work has been carried out within the framework of the Coordinated Research Project F22078 organized by the International Atomic Energy Agency (IAEA). | ANR-11-LABX-0018,IRON,Radiopharmaceutiques Innovants en Oncologie et Neurologie(2011)
International audience
اظهر المزيد [+] اقل [-]إنجليزي. We present a detailed investigation on the coordination chemistry of [nat/90Y]Y3+ and [nat/177Lu]Lu3+ with the new acyclic chelator H4CHXOITAPA. This octadentate chelator forms nine-coordinated Y3+ and Lu3+ complexes thanks to the coordination of a water molecule, as demonstrated by the X-ray structure of [Y(HCHXOITAPA)(H2O)] and 1H, 13C, and 89Y NMR studies in solution. These complexes display slightly higher thermodynamic stabilities compared with those of the known H4CHXOCTAPA and H4OCTAPA chelators, reaching log KYL and log KLuL values of 21.24(5) and 21.96(1), respectively. Kinetic studies indicate that these complexes dissociate mainly through the spontaneous and proton-assisted pathways at pH 7.4. The chelator can be readily radiolabeled with [90Y]Y3+ and [177Lu]Lu3+ at room temperature in 10 min. The radio-complexes are stable in human serum at 37 degrees C, in contrast with the analogues of the known H4CHXOCTAPA and H4OCTAPA chelators, which experience significant dissociation under these conditions. Thus, the H4CHXOITAPA chelator represents the most promising candidate among the H4OCTAPA family for the development of 90Y- and 177Lu-based radiopharmaceuticals.
اظهر المزيد [+] اقل [-]الكلمات المفتاحية الخاصة بالمكنز الزراعي (أجروفوك)
المعلومات البيبليوغرافية
تم تزويد هذا السجل من قبل Institut national de la recherche agronomique