The use of cationic metals in the form of a chelate comprising a metallic cation and one or more ligands in biological imaging such as cellular imaging is well-known. Chelates of trivalent rare-earth elements such as lanthanide cations (Ln3+) have attracted special attention in medical imaging due to their optical properties.
Existing ligands and lanthanide chelates have limitations impairing their use in photoluminescence in vitro or in vivo imaging studies. Some of existing complexes may have for example insufficient complexation strength (e.g. DTPA, EDTA), limited brightness, and/or cannot be easily functionalized (e.g., TACN). Therefore, there is a need for ligands with improved complexation properties, improved brightness and/or which can easily be functionalized.
The technology developed by the researchers relates to pyclen-based macrocyclic ligands (general scaffold below) which chelate efficiently Lanthanide cations and can be use in imaging, preferably by luminescence under one- or two- photons excitation.
This technology can be used especially in medical imaging in vivo or in vitro, molecular imaging, cellular imaging and/or bioassays imaging such as fluoro-immunoassays.
UMR 6521 - CEMCA
Equipe Chélates Azotés : Santé et Matériaux
EP : EP18305380.0 - filed on the 03-30-2018
WO - EP,US