4.5 Article

Iminosugar Analogues of Phosphatidyl Inositol as Potential Inhibitors of Protein Kinase B (Akt)

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

  1. CINMPIS Consortium
  2. Alsisan Programme [E07D400786BR]

向作者/读者索取更多资源

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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