Peer-Reviewed Journal Details
Mandatory Fields
Zhou J;Negi A;Mirallai SI;Warta R;Herold-Mende C;Carty MP;Ye XS;Murphy PV;
2019
March
Bioorganic Chemistry
N-Alkyl-1,5-dideoxy-1,5-imino-l-fucitols as fucosidase inhibitors: Synthesis, molecular modelling and activity against cancer cell lines.
Published
Optional Fields
84
1,5-Dideoxy-1,5-imino-l-fucitol (1-deoxyfuconojirimycin, DFJ) is an iminosugar that inhibits fucosidases. Herein, N-alkyl DFJs have been synthesised and tested against the ¿-fucosidases of T. maritima (bacterial origin) and B. taurus (bovine origin). The N-alkyl derivatives were inactive against the bacterial fucosidase, while inhibiting the bovine enzyme. Docking of inhibitors to homology models, generated for the bovine and human fucosidases, was carried out. N-Decyl-DFJ was toxic to cancer cell lines and was more potent than the other N-alkyl DFJs studied.
1090-2120
10.1016/j.bioorg.2018.12.003
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