Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies
Bello, Claudia; Cea, Michele; Dal Bello, Giovanna; Garuti, Anna; Rocco, Ilaria; Cirmena, Gabriella; Moran, Eva; Nahimana, Aimable; Duchosal, Michel A.; Fruscione, Floriana; Pronzato, Paolo; Grossi, Francesco; Patrone, Franco; Ballestrero, Alberto; Dupuis, Marc; Sordat, Bernard; Nencioni, Alessio; Vogel, Pierre
2010
Abstract
Novel alpha-mannosidase inhibitors of the type (2R,3R,4S)-2-({[(1R)-2- hydroxy-1-arylethyl]amine}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. (C) 2010 Elsevier Ltd. All rights reserved.
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Title
Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies
Author(s)
Bello, Claudia ; Cea, Michele ; Dal Bello, Giovanna ; Garuti, Anna ; Rocco, Ilaria ; Cirmena, Gabriella ; Moran, Eva ; Nahimana, Aimable ; Duchosal, Michel A. ; Fruscione, Floriana ; Pronzato, Paolo ; Grossi, Francesco ; Patrone, Franco ; Ballestrero, Alberto ; Dupuis, Marc ; Sordat, Bernard ; Nencioni, Alessio ; Vogel, Pierre
Published in
Bioorganic & Medicinal Chemistry
Volume
18
Pages
3320-3334
Date
2010
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LGSA
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Scientific production and competences > SB - School of Basic Sciences > SB Archives > LGSA - Laboratory of Glycochemistry and Asymmetric Synthesis
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Published
Peer-reviewed publications
Work produced at EPFL
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Record creation date
2011-12-16