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To date, the key approach in optimizing the pharmacological profile of antitumor drugs is delivery to validated biological targets (receptors, biomarkers, antigens, etc.). Among the targeting drug delivery to the liver, the strategy of creating specific compounds to asialoglycoprotein receptor takes leading roles [1]. Similar developments are also being made with drugs for treating hepatocellular carcinoma [2]. Besides, glycoconjugated systems allows to improve significantly the pharmacological profile of the initial molecules, which is especially important for natural triterpenoids. At present work, two covalent conjugates of betulin and N-acetylgalactosamine were synthesized and characterized. Initially, esters of betulin and 5-hexynoic acid were obtained. The subsequent interaction of azido derivatives of N-acetylgalactosamine with acetylenic moieties allowed selective conjugation of triterpenoid and specific monosaccharide, resulting in new potential bivalent ASGPR glycoconjugates.