ABSTRACT
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.
Subject(s)
Amides/chemistry , Chelating Agents/chemical synthesis , Heterocyclic Compounds, 1-Ring/chemistry , Chelating Agents/chemistry , Ligands , Molecular StructureABSTRACT
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.
Subject(s)
Contrast Media/chemistry , Magnetic Resonance Spectroscopy/standards , Magnetics , Organometallic Compounds/chemistry , Thulium/chemistry , Contrast Media/chemical synthesis , Magnetic Resonance Imaging , Magnetic Resonance Spectroscopy/methods , Molecular Structure , Organometallic Compounds/chemical synthesis , Reference StandardsABSTRACT
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.
