Bioorthogonal chemistry using transition metal catalysts (TMCs) is emerging as a promising strategy for drug delivery. In this strategy, deactivated caged prodrugs are bioorthogonally transformed by TMCs into their active form, to modulate cell bioprocesses. Several bioorthogonal TMCs have been developed including palladium, ruthenium, and iron porphyrin complexes. Among them, ruthenium catalysts result exemplary candidates due to their high turnover number, reduced toxicity and their high biorthogonality. These ruthenium complexes, however, are very selective to catalyze the deprotection of allyl-carbamate masked molecules, which can limit the design of prodrugs. Here we present different strategies to design stable allyl carbamate-based prodrugs able to be reactivate rapidly by ruthenium bioorthogonal catalysts and exert therapeutic activity in cells.

Metal-mediated catalysts for bioorthogonal therapeutics

256th National Meeting (2018)

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