2. Academic Validation
  3. Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase

Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase

  • Bioorg Med Chem Lett. 2006 Jul 15;16(14):3740-4. doi: 10.1016/j.bmcl.2006.04.046.
Sheela A Thomas 1,  Tongmei Li,  Keith W Woods,  Xiaohong Song,  Garrick Packard,  John P Fischer,  Robert B Diebold,  Xuesong Liu,  Yan Shi,  Vered Klinghofer,  Eric F Johnson,  Jennifer J Bouska,  Amanda Olson,  Ran Guan,  Shayna R Magnone,  Kennan Marsh,  Yan Luo,  Saul H Rosenberg,  Vincent L Giranda,  Qun Li
Affiliations

Affiliation

  • 1 Cancer Research, Department R47S, AP10 Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064, USA. [email protected]
PMID: 16678413 DOI: 10.1016/j.bmcl.2006.04.046
Abstract

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.

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