[natY/90Y]Yttrium and [natLu/177Lu]Lutetium Complexation by Rigid H4OCTAPA Derivatives. Effect of Ligand Topology.

IF 3.9 2区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Fátima Lucio-Martínez, Balázs Szilágyi, Rocío Uzal-Varela, Paulo Pérez-Lourido, David Esteban-Gómez, Nicolas Lepareur, Gyula Tircsó, C Platas-Iglesias
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引用次数: 0

Abstract

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 ºC, 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.

[natY/90Y]钇与[natLu/177Lu]镥的刚性H4OCTAPA衍生物络合。配体拓扑的影响。
本文详细研究了[nat/90Y]Y3+和[nat/177Lu]Lu3+与新型无环螯合剂H4CHXOITAPA的配位化学性质。[Y(HCHXOITAPA)(H2O)]的x射线结构和溶液中的1H、13C和89Y核磁共振研究表明,由于水分子的配位,该十八齿螯合剂形成了九配位的Y3+和Lu3+配合物。与已知的H4CHXOCTAPA和H4OCTAPA螯合剂相比,这些配合物表现出稍高的热力学稳定性,其logkyl和logklul分别达到21.24(5)和21.96(1)。动力学研究表明,这些配合物在pH值7.4时主要通过自发和质子辅助途径解离。该螯合剂可以在室温下10分钟内用[90Y]Y3+和[177Lu]Lu3+进行放射性标记。37℃时,放射性配合物在人血清中是稳定的,而已知的H4CHXOCTAPA和H4OCTAPA螯合剂的类似物在这些条件下会发生明显的解离。因此,H4CHXOITAPA螯合剂代表了H4OCTAPA家族中最有希望用于开发90Y-和177lu基放射性药物的候选物。
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来源期刊
Chemistry - A European Journal
Chemistry - A European Journal 化学-化学综合
CiteScore
7.90
自引率
4.70%
发文量
1808
审稿时长
1.8 months
期刊介绍: Chemistry—A European Journal is a truly international journal with top quality contributions (2018 ISI Impact Factor: 5.16). It publishes a wide range of outstanding Reviews, Minireviews, Concepts, Full Papers, and Communications from all areas of chemistry and related fields. Based in Europe Chemistry—A European Journal provides an excellent platform for increasing the visibility of European chemistry as well as for featuring the best research from authors from around the world. All manuscripts are peer-reviewed, and electronic processing ensures accurate reproduction of text and data, plus short publication times. The Concepts section provides nonspecialist readers with a useful conceptual guide to unfamiliar areas and experts with new angles on familiar problems. Chemistry—A European Journal is published on behalf of ChemPubSoc Europe, a group of 16 national chemical societies from within Europe, and supported by the Asian Chemical Editorial Societies. The ChemPubSoc Europe family comprises: Angewandte Chemie, Chemistry—A European Journal, European Journal of Organic Chemistry, European Journal of Inorganic Chemistry, ChemPhysChem, ChemBioChem, ChemMedChem, ChemCatChem, ChemSusChem, ChemPlusChem, ChemElectroChem, and ChemistryOpen.
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