Glucose-based analogues of phosphatidylinositol 3-phosphate were straightforwardly synthesised from 2,3,4,6-tetra-O-acetyl-D-glucosyl bromide as protein kinase B (PKB/Akt) inhibitors. β-D-Glucuronyl diethyl phosphoramidate was identified as a promising hit through biological screening in two different cellular systems. In addition, RNA interference experiments (siRNA) provide evidence of the ability of the compound to exert biological effects specifically through Akt signalling. © 2009 Elsevier Ltd. All rights reserved.
Cipolla, L., Redaelli, C., Granucci, F., Zampella, G., Zaza, A., Chisci, R., et al. (2010). Straightforward synthesis of novel Akt inhibitors based on a glucose scaffold. CARBOHYDRATE RESEARCH, 345(10), 1291-1298 [10.1016/j.carres.2009.12.013].
Straightforward synthesis of novel Akt inhibitors based on a glucose scaffold
CIPOLLA, LAURA FRANCESCA
;GRANUCCI, FRANCESCA;ZAMPELLA, GIUSEPPE;ZAZA, ANTONIO;CHISCI, RICCARDO;NICOTRA, FRANCESCO
2010
Abstract
Glucose-based analogues of phosphatidylinositol 3-phosphate were straightforwardly synthesised from 2,3,4,6-tetra-O-acetyl-D-glucosyl bromide as protein kinase B (PKB/Akt) inhibitors. β-D-Glucuronyl diethyl phosphoramidate was identified as a promising hit through biological screening in two different cellular systems. In addition, RNA interference experiments (siRNA) provide evidence of the ability of the compound to exert biological effects specifically through Akt signalling. © 2009 Elsevier Ltd. All rights reserved.
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