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Synthetic strategy for preparation of a folate corrole DOTA heterobimetallic Cu–Gd complex as a potential bimodal contrast agent in medical imaging
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2015-11-22 10:00:12
Nicolas Desbois, Clément Michelin, Yi Chang, Vasile Stupar, Mylène Bonnaud, Sandrine Pacquelet, Claude P. Gros

An efficient sequential route to synthesize heterobimetallic complexes is reported herein. A folate, Cu corrole, Gd DOTA complex that addresses the requirements of a potential contrast agent (CA) for bimodal imaging (e.g., MRI/PET) is reported. The over-expression of the folate receptor in a variety of malignant tumors, along with its limited expression in healthy tissues, makes this an attractive tumor-specific molecular target. Synthesis of a bimetallic ligand potentially targeting the folate receptor, was easily achieved in only a few steps. Interestingly, preliminary studies showed that the relaxivity of the folic heterobimetallic derivative was higher in comparison to a clinically used Gd DOTA MRI contrast agent. Their radiocomplexes may be useful as an in vitro tool and for in vivo tumor diagnosis by using, for example, PET imaging.

中文翻译:

合成叶酸腐蚀剂DOTA异双金属Cu-Gd络合物作为医学影像中潜在的双峰造影剂的合成策略

本文报道了合成异双金属配合物的有效顺序路线。据报道,叶酸,铜,铜,Gd DOTA复合物可满足双峰成像(例如MRI / PET)潜在的造影剂(CA)的要求。叶酸受体在多种恶性肿瘤中的过度表达及其在健康组织中的有限表达,使其成为有吸引力的肿瘤特异性分子靶标。仅需几个步骤即可轻松实现潜在靶向叶酸受体的双金属配体的合成。有趣的是,初步研究表明,叶叶异双金属衍生物的弛豫性高于临床使用的Gd DOTA MRI造影剂。它们的放射性复合物可以用作体外工具,并可以通过使用例如PET成像进行体内肿瘤诊断。
更新日期:2015-11-23
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