Synthetic strategy for preparation of a folate corrole DOTA heterobimetallic Cu–Gd complex as a potential bimodal contrast agent in medical imaging. Issue 51 (23rd December 2015)

• Record Type: Journal Article
• Authors: Desbois, Nicolas; Michelin, Clément; Chang, Yi; Stupar, Vasile; Bonnaud, Mylène; Pacquelet, Sandrine; Gros, Claude P.
• Is Part Of: Tetrahedron letters. Volume 56:Issue 51(2015)
• Page Start: 7128
• Page End: 7131
• Publication Date: 2015-12-23
• Subjects: Corrole -- Gadolinium -- Copper -- Imaging agent -- Folic acid; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2015.11.032
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Abstract: 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.