Masking Strategies for the Bioorthogonal Release of Anticancer Glycosides

Belén Rubio-ruiz, Thomas L. Bray, Ana Perez-Lopez, Asier Unciti-broceta

Research output: Chapter in Book/Report/Conference proceedingChapter


Significant progress in the bioorthogonal field has resulted in the advent of a new type of prodrug: bioorthogonal prodrugs, i.e. metabolically stable precursors of therapeutic agents that are specifically activated by non-native, non-biological, non-perturbing physical or chemical stimuli. The application of such unique drug precursors in conjunction with their corresponding activating source is under preclinical experimentation as a novel way to elicit site-specific activation of cytotoxic drugs, with particular emphasis on anticancer glycosides. In this chapter, the strategies developed for the masking and bioorthogonal release of cytotoxic nucleosides using benign electromagnetic radiations, biocompatible click chemistry and bioorthogonal organometallic (BOOM) catalysis will be discussed in detail.
Original languageEnglish
Title of host publicationCoupling and Decoupling of Diverse Molecular Units in Glycosciences
EditorsZbigniew J. Witczak, Roman Bielski
PublisherSpringer International Publishing
ISBN (Electronic)978-3-319-65587-1
ISBN (Print)978-3-319-65586-4
Publication statusPublished - 21 Nov 2017


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