ИСТИНА

Asialoglycoprotein receptor (ASGP-R) is a transmembrane protein that predominantly found on the surface of parenchymal liver cells. ASGPR is a promising target for targeted drug delivery in hepatocytes and liver tumor cells. It is known that most of the ASGPR ligands contain galactose- n-acetylgalactosamine residues, while non-carbohydrate structures are poorly studied. Recently, we have observed that quinolines containing a carboxyl group in the fourth position are able to effectively bind to ASGPR. Azide-alkyne copper-catalyzed cycloaddition reaction is a convenient method of modification functional groups of biological active compounds. In order to use this method, it is necessary to add azido group or terminal triple bond into a molecule. Here we report a synthetic approach to novel ethynyl substituted 3-hydroxyguinoline-4-carboxylic acids.