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

Details

Serval ID
serval:BIB_FE0F7F1D0119
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies.
Journal
Bioorganic & medicinal chemistry
Author(s)
Bello C., Cea M., Dal Bello G., Garuti A., Rocco I., Cirmena G., Moran E., Nahimana A., Duchosal M.A., Fruscione F., Pronzato P., Grossi F., Patrone F., Ballestrero A., Dupuis M., Sordat B., Nencioni A., Vogel P.
ISSN
1464-3391 (Electronic)
ISSN-L
0968-0896
Publication state
Published
Issued date
01/05/2010
Peer-reviewed
Oui
Volume
18
Number
9
Pages
3320-3334
Language
english
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Abstract
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.

Keywords
Antineoplastic Agents/chemical synthesis, Antineoplastic Agents/chemistry, Antineoplastic Agents/pharmacology, Cell Line, Tumor, Cell Proliferation/drug effects, Hematologic Neoplasms, Humans, Inhibitory Concentration 50, Molecular Structure, Neoplasms, Teprotide/chemical synthesis, Teprotide/chemistry, Teprotide/pharmacology, alpha-Mannosidase/antagonists & inhibitors
Pubmed
Web of science
Create date
18/05/2010 16:34
Last modification date
20/08/2019 17:28
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