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

Détails

ID Serval
serval:BIB_FE0F7F1D0119
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies.
Périodique
Bioorganic & medicinal chemistry
Auteur⸱e⸱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
Statut éditorial
Publié
Date de publication
01/05/2010
Peer-reviewed
Oui
Volume
18
Numéro
9
Pages
3320-3334
Langue
anglais
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't
Publication Status: ppublish
Résumé
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.

Mots-clé
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
Création de la notice
18/05/2010 16:34
Dernière modification de la notice
20/08/2019 17:28
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