Vitamin B12 has been proposed as a natural vector for in vivo delivery of biologically active compounds. Most synthetic methodologies leading to vitamin B12 conjugates involved functionalization at the 5' position via either carbamate-based linkages or using copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) leading to stable conjugates that are not cleaved within the cell. We have developed a novel vitamin B12 derivative suitably tailored for disulfide-based conjugation that can undergo cleavage in the presence of glutathione (GSH) - the most abundant thiol in mammalian cells. This active compound is simple to prepare and allows for direct disulfide-based attachment of therapeutic cargos.
Mendeley saves you time finding and organizing research
Choose a citation style from the tabs below