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Tetrazine-mediated bioorthogonal prodrug–prodrug activation

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Original languageEnglish
Pages (from-to)7198-7203
JournalChemical Science
Issue number36
Early online date12 Jul 2018
Publication statusE-pub ahead of print - 12 Jul 2018


The selective and biocompatible activation of prodrugs within complex biological systems remains a key challenge in medical chemistry and chemical biology. Herein we report, for the first time, a dual prodrug activation strategy that fully satisfies the principle of bioorthogonality by the symbiotic formation of two active drugs without the generation of any by-products. This dual and traceless prodrug activation strategy takes advantage of the INVDA chemistry of tetrazines (here a prodrug), generating a pyridazine-based miR21 inhibitor and the anti-cancer drug camptothecin, and offers a new concept in prodrug activation.

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