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Iminosugar Analogues of Phosphatidyl Inositol as Potential Inhibitors of Protein Kinase B (Akt)
Author(s) -
Orsato Alexandre,
Barbagallo Emanuela,
Costa Barbara,
Olivieri Sandro,
De Gioia Luca,
Nicotra Francesco,
La Ferla Barbara
Publication year - 2011
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201100452
Subject(s) - iminosugar , chemistry , protein kinase b , docking (animal) , enzyme , biochemistry , virtual screening , kinase , stereochemistry , combinatorial chemistry , phosphorylation , drug discovery , medicine , nursing
A small virtual library of iminosugar derivatives was evaluated by docking experiments carried out by sampling a protein region corresponding to the phosphoinositide binding site of the PH domain of Akt. Four compounds were selected and efficiently synthesised from a common precursor. All compounds were subjected to preliminary biological evaluation on purified enzyme, and – among them – compound 9 exhibited the best inhibitory activity.