COA of Formula: C8H6BrNIn 2020 ,《Regioselective 3-O-Substitution of Unprotected Thiodigalactosides: Direct Route to Galectin Inhibitors》 was published in Chemistry – A European Journal. The article was written by Vasicek, Tomas; Spiwok, Vojtech; Cerveny, Jakub; Petraskova, Lucie; Bumba, Ladislav; Vrbata, David; Pelantova, Helena; Kren, Vladimir; Bojarova, Pavla. The article contains the following contents:
The synthesis of tailored bioactive carbohydrates usually comprises challenging (de)protection steps, which lowers synthetic yields and increases time demands. We present here a regioselective single-step introduction of benzylic substituents at 3-hydroxy groups of β-D-galactopyranosyl-(1→1)-thio-β-D-galactopyranoside (TDG) employing dibutyltin oxide in good yields. These glycomimetics act as inhibitors of galectins-human lectins, which are bio-medically attractive targets for therapeutic inhibition in, for example, cancerogenesis. The affinity of the prepared glycomimetics to galectin-1 and galectin-3 was studied in enzyme-linked immunosorbent (ELISA)-type assays and their potential to inhibit galectin binding on the cell surface was shown. We used our original in vivo biotinylated galectin constructs for easy detection by flow cytometry. The results of the biol. experiments were compared with data from mol. modeling with both galectins. The present work reveals a facile and elegant synthetic route for the preparation of TDG-derived glycomimetics that exhibit differing selectivity and affinity to galectins depending on the choice of 3-O-substitution. The experimental part of the paper was very detailed, including the reaction process of 4-Cyanobenzyl bromide(cas: 17201-43-3COA of Formula: C8H6BrN)
4-Cyanobenzyl bromide(cas: 17201-43-3) can reacts with 2H-tetrazole in the presence of KOH to yield 4-[(2H-tetra-zol-2-yl)methyl]benzonitrile. And it may be used in the synthesis of ligands containing a chelating pyrazolyl-pyridine group with a pendant aromatic nitrile.COA of Formula: C8H6BrN
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts