6533b821fe1ef96bd127c427
RESEARCH PRODUCT
Novel heterobimetallic radiotheranostic: preparation, activity, and biodistribution.
Semra TasanFranck DenatFernanda MarquesLurdes GanoCélia FernandesMaria Paula Cabral CampelloMichel PicquetEwen BodioPierre Le GendreLouis AdriaenssensQiang LiuFilipa MendesFanny Chaux-picquetsubject
BiodistributionStereochemistryCell SurvivalPhosphinesIn vitro cytotoxicitychemistry.chemical_elementBiochemistryRutheniumMetalHeterocyclic Compounds 1-RingMiceIn vivoCoordination ComplexesCell Line TumorDrug DiscoveryAnimalsHumansTissue DistributionGeneral Pharmacology Toxicology and PharmaceuticsSolubilityPharmacologyChemistryLigandOrganic ChemistryWaterRutheniumvisual_artPhosphorus atomIsotope Labelingvisual_art.visual_art_mediumMolecular MedicineRadiopharmaceuticalsdescription
A novel Ru(II) (arene) theranostic complex is presented. It is based on a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid macrocycle bearing a triarylphosphine and can be tracked in vivo by using the γ emission of (153) Sm atoms. Notably, the heteroditopic ligand can be selectively metalated with ruthenium at the phosphorus atom despite the presence of other functionalities that are prone to metal coordination. Subsequent labeling with radionuclides such as (153) Sm can then be performed easily. The resulting heterobimetallic complex exhibits favorable solubility and stability properties in biologically relevant media. It also shows in vitro cytotoxicity in line with that expected for this type of metallodrug, and is nontoxic to the organism as a whole. As a proof of concept, initial studies in healthy mice were performed to obtain information about the uptake, biodistribution, and excretion of the radiolabeled complex.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2014-01-21 | ChemMedChem |