Cyclative cleavage of an amine-carbamate self-immolative spacer to deliver a hydroxyl cargo was inhibited by the spacer derivatisation with a phosphate monoester handle. This trifunctional spacer was installed in a model anticancer prodrug which showed a fast drug release only when incubated with both a protease and a phosphatase enzymes.
A Trifunctional Self-Immolative Spacer Enables Drug Release with Two Non-Sequential Enzymatic Cleavages / A. DAL CORSO, S. Arosio, N. Arrighetti, P. Perego, L. Belvisi, L. Pignataro, C. Gennari. - In: CHEMICAL COMMUNICATIONS. - ISSN 1359-7345. - 57:63(2021 Aug 14), pp. 7778-7781. [10.1039/D1CC02895B]
A Trifunctional Self-Immolative Spacer Enables Drug Release with Two Non-Sequential Enzymatic Cleavages
A. DAL CORSO
Primo
;L. Belvisi;L. PignataroPenultimo
;C. Gennari
Ultimo
2021
Abstract
Cyclative cleavage of an amine-carbamate self-immolative spacer to deliver a hydroxyl cargo was inhibited by the spacer derivatisation with a phosphate monoester handle. This trifunctional spacer was installed in a model anticancer prodrug which showed a fast drug release only when incubated with both a protease and a phosphatase enzymes.
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