RESUMEN
Improved LIPOCEST MRI contrast agents with highly shifted intraliposomal water protons were prepared by entrapping neutral polynuclear Tm(III)-based paramagnetic shift reagents in phospholipidic vesicles.
Asunto(s)
Medios de Contraste/química , Espectroscopía de Resonancia Magnética/normas , Magnetismo , Compuestos Organometálicos/química , Tulio/química , Medios de Contraste/síntesis química , Imagen por Resonancia Magnética , Espectroscopía de Resonancia Magnética/métodos , Estructura Molecular , Compuestos Organometálicos/síntesis química , Estándares de ReferenciaRESUMEN
We have synthesized rigid analogues of combretastatin bearing a furan ring in place of the olefinic bridge. These compounds are cytotoxic at nanomolar concentrations in neuroblastoma cells, display a similar structure-activity relationship compared to combretastatin A4, and inhibit tubulin polymerization. We also show that the furan ring can be further functionalized. Thus, it is possible that combretafurans could act as scaffolds for the development of dual-action antitumoral agents.
Asunto(s)
Anisoles/síntesis química , Anisoles/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Bibencilos/síntesis química , Bibencilos/farmacología , Furanos/química , Neuroblastoma/tratamiento farmacológico , Estilbenos/síntesis química , Estilbenos/farmacología , Anisoles/química , Antineoplásicos/química , Bibencilos/química , Muerte Celular/efectos de los fármacos , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Estilbenos/química , Relación Estructura-Actividad , Tubulina (Proteína)/efectos de los fármacosRESUMEN
Efficient routes to DOTA-monoamide ligands bearing amino, hydroxyl, aldehyde and maleimido groups are described. These functional groups, which can be spaced at will from the coordination cage, will readily react with suitable groups of targeting moieties. Bioconjugates obtained in this way can be used for diagnostic imaging and therapeutic applications.