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. 2016 Mar 15;26(6):1546-1549.
doi: 10.1016/j.bmcl.2016.02.017. Epub 2016 Feb 9.

A second-generation ferrocene-iminosugar hybrid with improved fucosidase binding properties

Audrey Hottin  1 , Amandine Scandolera  2 , Laurent Duca  2 , Daniel W Wright  3 , Gideon J Davies  3 , Jean-Bernard Behr  4
Affiliations

A second-generation ferrocene-iminosugar hybrid with improved fucosidase binding properties

Audrey Hottin et al. Bioorg Med Chem Lett. .

Abstract

The synthesis and the biological evaluation of a new ferrocenyl-iminosugar conjugate designed for fucosidase inhibitory and anticancer activity is described. The compound showed strong affinity for fucosidase from bovine kidney (Ki=23 nM) and from Bacteroides thetaiotaomicron (Ki=150 nM), displaying a 10-fold tighter binding affinity for these enzymes than the previous analogs. The interaction pattern that improves binding has been evaluated through structural analysis of the inhibitor-enzyme complex. The ferrocenyl-iminosugar exhibits significant anticancer activity on MDA-MB-231 and SK-MEL28 cell lines at 100 μM.

Keywords: Anticancer; Ferrocene; Fucosidase; Iminosugars; Inhibitors.

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