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

被引：23

作者：

Bello, Claudia ^{[1
]}

Cea, Michele ^{[3
]}

Dal Bello, Giovanna ^{[2
]}

Garuti, Anna ^{[3
]}

Rocco, Ilaria ^{[3
]}

Cirmena, Gabriella ^{[3
]}

Moran, Eva ^{[3
]}

Nahimana, Aimable ^{[5
]}

Duchosal, Michel A. ^{[5
]}

Fruscione, Floriana ^{[4
]}

Pronzato, Paolo ^{[2
]}

Grossi, Francesco ^{[2
]}

Patrone, Franco ^{[3
]}

Ballestrero, Alberto ^{[3
]}

Dupuis, Marc ^{[1
]}

Sordat, Bernard ^{[1
]}

Nencioni, Alessio ^{[3
]}

Vogel, Pierre ^{[1
]}

机构：

[1] Ecole Polytech Fed Lausanne, Lab Glycochem & Asymmetr Synth LGSA, CH-1015 Lausanne, Switzerland

[2] Natl Inst Canc Res, I-16132 Genoa, Italy

[3] Univ Genoa, Dept Internal Med, I-16126 Genoa, Italy

[4] Univ Genoa, Dept Expt Med, I-16126 Genoa, Italy

[5] Univ Hosp CHUV, Serv Hematol, Lausanne, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 09期

基金：

瑞士国家科学基金会;

关键词：

Glycosylation; alpha-Mannosidase inhibitors; Antiproliferative effects; Cell cycle; Haematological malignances; ENDOPLASMIC-RETICULUM; HUMAN GLIOBLASTOMA; CELL SURVIVAL; CANCER; GLYCOSYLATION; SWAINSONINE; LYMPHOMA; GROWTH; BCL-2; CYTOTOXICITY;

D O I：

10.1016/j.bmc.2010.03.009

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

Novel alpha-mannosidase inhibitors of the type (2R,3R,4S)-2-({[(1R)-2- hydroxy-1-arylethyl]amine}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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：3320 / 3334

页数：15

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