Publications by authors named "Trevor K Harrison"
Article Synopsis
- - A new treatment approach for inflammatory diseases like rheumatoid arthritis focuses on specifically targeting the JAK1 pathway, which could lead to better outcomes.
- - Researchers identified a new binding structure while studying existing pan-JAK inhibitors, which showed a good ability to accept various chemical modifications.
- - The study resulted in highly effective JAK1 inhibitors with strong performance in cell tests and selective action over JAK2, supported by X-ray crystallography to optimize their design.
Potent small molecule inhibitors of spleen tyrosine kinase (Syk).
Bioorg Med Chem Lett
September 2003
A series of oxindoles demonstrating inhibition of the phosphorylation of biotinylated substrates of Syk and IgE/Fc epsilon RI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC(50)=5 nM, EC(50)=1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar Surface Area was lowered to <110 A(2), leading to the identification of amide 32 (IC(50)=145 nM, EC(50)=100 nM).
View Article and Find Full Text PDFThe utilization and impact of parallel synthesis on lead exploration around initial hit oxindole (1) are described. The emergent SAR, analogue design and functional impact will also be detailed.
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