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Novel 2-[(benzylamino)methyl]pyrrolidine-3,4-diol derivatives as alpha-mannosidase inhibitors and with antitumor activities against hematological and solid malignancies.
Bello, Claudia; Cea, Michele; Dal Bello, Giovanna; Garuti, Anna; Rocco, Ilaria; Cirmena, Gabriella; Moran, Eva; Nahimana, Aimable; Duchosal, Michel A; Fruscione, Floriana; Pronzato, Paolo; Grossi, Francesco; Patrone, Franco; Ballestrero, Alberto; Dupuis, Marc; Sordat, Bernard; Nencioni, Alessio; Vogel, Pierre.
Afiliación
  • Bello C; Laboratory of Glycochemistry and Asymmetric Synthesis (LGSA), Ecole Polytechnique Fédérale de Lausanne (EPFL), Batochime, CH-1015 Lausanne, Switzerland. claudia.bello@epfl.ch
Bioorg Med Chem ; 18(9): 3320-34, 2010 May 01.
Article en En | MEDLINE | ID: mdl-20346684
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.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Teprotido / Neoplasias Hematológicas / Alfa-Manosidasa / Neoplasias Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Teprotido / Neoplasias Hematológicas / Alfa-Manosidasa / Neoplasias Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2010 Tipo del documento: Article País de afiliación: Suiza Pais de publicación: Reino Unido