Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377938 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
Based on lead compounds 2 and 3 a series of 3,5-disubstituted pyridines have been designed and evaluated for inhibition of AKT/PKB. Modifications at the 3 position of the pyridine ring led to a number of potent compounds with improved physical properties, resulting in the identification of 11g as a promising, orally active Akt inhibitor. The synthesis, structure–activity relationship studies, and pharmacokinetic data are presented in this paper.
Graphical abstractBased on lead compounds 2 and 3 a series of 3,5-disubstituted pyridines have been designed and evaluated for inhibition of AKT/PKB. Modifications at the 3 position of the pyridine ring led to a number of potent compounds with improved physical properties, resulting in the identification of 11g as a promising, orally active AKT inhibitor. The synthesis, structure–activity relationship studies, and pharmacokinetic data are presented in this paper.Figure optionsDownload full-size imageDownload as PowerPoint slide