Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as α-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies

Claudia Bello, Michele Cea, Giovanna Dal Bello, Anna Garuti, Ilaria Rocco, Gabriella Cirmena, Eva Moran, Aimable Nahimana, Michel A. Duchosal, Floriana Fruscione, Paolo Pronzato, Francesco Grossi, Franco Patrone, Alberto Ballestrero, Marc Dupuis, Bernard Sordat, Alessio Nencioni, Pierre Vogel

Research output: Contribution to journalArticlepeer-review

Abstract

Novel α-mannosidase inhibitors of the type (2R,3R,4S)-2-({[(1R)-2-hydroxy-1-arylethyl]amino}methyl)pyrrolidine-3,4-diol have been prepared and assayed for their anticancer activities. Compound 30 with the aryl group = 4-trifluoromethylbiphenyl inhibits the proliferation of primary cells and cell lines of different origins, irrespective of Bcl-2 expression levels, inducing a G2/Mcell cycle arrest and by modification of genes involved in cell cycle progression and survival.

Original languageEnglish
Pages (from-to)3320-3334
Number of pages15
JournalBioorganic and Medicinal Chemistry
Volume18
Issue number9
DOIs
Publication statusPublished - May 1 2010

Keywords

  • α-Mannosidase inhibitors
  • Antiproliferative effects
  • Cell cycle
  • Glycosylation
  • Haematological malignances

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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