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
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
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 15:34
Last modification date
20/08/2019 16:28