- Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies.
Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies.
Bioorganic & medicinal chemistry (2010-03-30)
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
PMID20346684
摘要
Novel alpha-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.
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