Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369593 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
Dual PI3Kγ/δ inhibitors have recently been shown to be suitable targets for inflammatory and respiratory diseases. In a recent study we described the discovery of selective PI3Kγ inhibitors based on a triazolopyridine scaffold. Herein, we describe the elaboration of this structural class into dual PI3Kγ/δ inhibitors with excellent selectivity over the other PI3K isoforms and the general kinome. Structural optimization led to the identification of two derivatives which showed significant efficacy in an acute model of lung inflammation.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Katie Ellard, Mihiro Sunose, Kathryn Bell, Nigel Ramsden, Giovanna Bergamini, Gitte Neubauer,