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Library of a new class of C‐1 monosulfated saccharide derivatives derived from D‐fructofuranose have been synthesized as potential GnT‐I inhibitors. To increase stability of originally proposed thioglycosides, the compounds were oxidized to sulfones bearing three different aglycons; ethyl, 2‐methyl propyl (isopropyl) and phenyl. Here we present molecular modelling, synthesis and biological assays of prepared compounds. [ABSTRACT FROM AUTHOR]

New potential transition state analogue inhibitors for N-acetylglucosyltransferases (GnTs) were synthesised. These compounds based on psico- and tagatofuranose (structure) scaffold contained a 2-thiophenyl-1-O-diethylphosphate moiety mimicking the proposed model of the transition state of the enzymatic reaction catalysed by N-acetylglucosyltransferases. The synthesised compounds as well as their precursors were fully characterised by NMR, optical rotation and mass techniques. Anomeric configuration of tagatofuranose derivatives was confirmed by X-ray crystallography. Two types of potential human glycosyltransferase (GnTs) inhibitors representing donor UDP-GlcNAc, assigned for biological assays on human GnTs, were prepared. [ABSTRACT FROM AUTHOR]