Synthesis of cluster galactosides with high affinity for the hepatic asialoglycoprotein receptor

…, GA van de Marel, JH Van Boom…

Index: Biessen, Erik A.L.; Beuting, Diana M.; Roelen, Harlof C.P.F.; Marel, Gijs A. van de; Boom, Jacques H. van; Berkel, Theo J.C. van Journal of Medicinal Chemistry, 1995 , vol. 38, # 9 p. 1538 - 1546

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Citation Number: 141

Abstract

O-(/3-~-galactopyranosyl) methyllmethyll-N~-[1-(6-methyladipyl)] glycinamide (4a), a cluster galactoside lacking the spacer. It is concluded that vicinal galactosyl moieties within a cluster galactoside are more optimal recognized by the galactose binding sites of the asialoglycoprotein receptor upon proper spacing. The most potent galactoside, TG (20&, may constitute an attractive targeting device for the specific delivery of drugs and/or genes ...