期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2014, 期 27, 页码 5962-5967出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201402664
关键词
Medicinal chemistry; Antitumor agents; Carbohydrates; Inhibitors; Enzymes; Phospholipids
资金
- Fondazione Cariplo [2011-0490]
New sulfoquinovose analogues of phosphatidylinositol 3-phosphate have been synthesised based on a sulfoquinovose scaffold as potential protein kinase B (PKB) inhibitors. The synthetic strategy involved the introduction into glucose of a thioacetate group at the 6-position and of an azide group at the anomeric position as precursors of the sulfonate and phosphoramidate moieties present in the final compounds. The synthesised compounds were tested in vitro on isolated PKB by means of ELISA assays and for their anti-proliferative activity against the human ovarian carcinoma cell line IGROV-1. Sulfoquinovose derivatives 2b and 2c showed inhibitory activity in the low micromolar range.
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