Lelieveldt, Lianne P. W. M. published the artcileVinylboronic acid-caged prodrug activation using click-to-release tetrazine ligation, Safety of Picolinonitrile, the main research area is vinylboronic acid cage prodrug click controlled release tetrazine ligation.
Bioorthogonal reactions can be performed selectively in the presence of any biol. functional group and are widely used to achieve site-selective chem. modifications of biomols. The click-to-release reaction is a bioorthogonal bond-cleavage variant that has gained much interest over the last few years. The bioorthogonal reaction between tetrazines and trans-cyclooctenes or vinyl ethers, for example, initiates the release of a small mol. immediately after the cycloaddition with tetrazines. Recently, our group reported that vinylboronic acids (VBAs) give exceptionally high reaction rates in the bioorthogonal inverse electron-demand Diels-Alder reaction with tetrazines that are substituted with boron-coordinating ligands. In the present study, we show that VBAs can be used in a click-to-release variant and demonstrate its bioorthogonality with a VBA-protected doxorubicin prodrug. We show that the cytotoxicity of doxorubicin is silenced by the attachment of the VBA, and activity can be largely restored upon the reaction with a tetrazine, inducing cell death.
Organic & Biomolecular Chemistry published new progress about Antitumor agents. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, Safety of Picolinonitrile.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts