| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369612 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Juan-Miguel Jimenez, Christopher Davis, Dean Boyall, Damien Fraysse, Ronald Knegtel, Luca Settimo, Stephen Young, Claire Bolton, Peter Chiu, Adam Curnock, Richele Rasmussen, Adam Tanner, Ian Ager,