The present work is dedicated to Professor Ladislav Petruš on the occasion of his 70th birthday.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 oxi-dized to sulfones bearing three different aglycons; ethyl, 2methyl propyl (isopropyl) and phenyl. Here we present molecular modelling, synthesis and biological assays of prepared compounds. Scheme 2. Reagent and Conditions: a) TBDMSCl, pyridine, À 20°C!r.t., overnight; b) DMTrCl, DMAP, pyridine, r.t. overnight; c) 1 M TBAF in THF, THF, r.t., 90 min; d) BnBr, DMF, NaH, 0°C!r.t., 2 h; e) CF 3 COOH, DCM, triethylsilane, r.t., 1.5-4 h. Scheme 3. Reagent and Conditions: a) SO 3 ⋅py complex, DCM, r.t., 48 h; b) 3chloroperbenzoic acid, DCM, 0°C!r.t., 0.5-1.5 h. Scheme 4. Reagent and Conditions: a) SO 3 .py complex, DCM, r.t., 48 h; b) cat. 10 % Pd/C, H 2 , MeOH, 2 h.