Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370396 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
Imidazo[1,5-a]quinoxalines were synthesized that function as irreversible Bruton’s tyrosine kinase (BTK) inhibitors. The syntheses and SAR of this series of compounds are presented as well as the X-ray crystal structure of the lead compound 36 in complex with a gate-keeper variant of ITK enzyme. The lead compound showed good in vivo efficacy in preclinical RA models.
Graphical abstractThe synthesis and structure–activity relationships for a series of imidazo[1,5-a]quinoxalines as irreversible inhibitors of BTK are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kyung-Hee Kim, Andreas Maderna, Mark E. Schnute, Martin Hegen, Shashi Mohan, Joy Miyashiro, Laura Lin, Evelyn Li, Sean Keegan, Jennifer Lussier, Christopher Wrocklage, Cheryl L. Nickerson-Nutter, Arthur J. Wittwer, Holly Soutter, Nicole Caspers,