By the same authors

From the same journal

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

Research output: Contribution to journalArticle

Published copy (DOI)

Author(s)

  • Audrey Hottin
  • Amandine Scandolera
  • Laurent Duca
  • Daniel W. Wright
  • Gideon J. Davies
  • Jean Bernard Behr

Department/unit(s)

Publication details

JournalBioorganic & Medicinal Chemistry Letters
DateAccepted/In press - 7 Feb 2016
DateE-pub ahead of print - 9 Feb 2016
DatePublished (current) - 15 Mar 2016
Issue number6
Volume26
Pages (from-to)1546-1549
Early online date9/02/16
Original languageEnglish

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 (K i =23nM) and from Bacteroides thetaiotaomicron (K i =150nM), 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 100μM.

    Research areas

  • Anticancer, Ferrocene, Fucosidase, Iminosugars, Inhibitors

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