Article ID Journal Published Year Pages File Type
1370396 Bioorganic & Medicinal Chemistry Letters 2011 6 Pages PDF
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

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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