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Bioorg Med Chem Lett. 2012 Jul 15;22(14):4645-9. doi: 10.1016/j.bmcl.2012.05.114. Epub 2012 Jun 6.

Structure-based optimization of aminopyridines as PKCθ inhibitors.

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  • 1Department of Chemistry at Vertex Pharmaceuticals (Europe) Ltd, 88 Milton Park, Abingdon OX14 4RY, United Kingdom.


The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin-3-yl)methanone 2 leading to compound 21 which significantly inhibits production of IL-2 in a mouse SEB-IL2 model.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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