TY - JOUR
T1 - Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as α-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies
AU - Bello, Claudia
AU - Cea, Michele
AU - Bello, Giovanna Dal
AU - Garuti, Anna
AU - Rocco, Ilaria
AU - Cirmena, Gabriella
AU - Moran, Eva
AU - Nahimana, Aimable
AU - Duchosal, Michel A.
AU - Fruscione, Floriana
AU - Pronzato, Paolo
AU - Grossi, Francesco
AU - Patrone, Franco
AU - Ballestrero, Alberto
AU - Dupuis, Marc
AU - Sordat, Bernard
AU - Nencioni, Alessio
AU - Vogel, Pierre
PY - 2010/5/1
Y1 - 2010/5/1
N2 - 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.
AB - 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.
KW - α-Mannosidase inhibitors
KW - Antiproliferative effects
KW - Cell cycle
KW - Glycosylation
KW - Haematological malignances
UR - http://www.scopus.com/inward/record.url?scp=77951207403&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=77951207403&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2010.03.009
DO - 10.1016/j.bmc.2010.03.009
M3 - Article
C2 - 20346684
AN - SCOPUS:77951207403
VL - 18
SP - 3320
EP - 3334
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 9
ER -