期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2011, 期 26, 页码 5012-5019出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201100452
关键词
Iminosugars; Enzymes; Inhibitors; PH domain; Docking; Glycomimetics; Drug design; Enzyme models
资金
- CINMPIS Consortium
- Alsisan Programme [E07D400786BR]
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.
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