Scientific Publications

Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction in β-Cells with Improved Aqueous Solubility.

Publication TypeJournal Article
AuthorsScully, SS, Tang AJ, Lundh M., Mosher CM, Perkins KM, and Wagner BK
AbstractWe previously reported the discovery of BRD0476 (1), a small molecule generated by diversity-oriented synthesis that suppresses cytokine-induced β-cell apoptosis. Herein, we report the synthesis and biological evaluation of 1 and analogues with improved aqueous solubility. By replacing naphthyl with quinoline moieties, we prepared active analogues with up to a 1400-fold increase in solubility from 1. In addition, we demonstrated that 1 and analogues inhibit STAT1 signal transduction induced by IFN-γ.
Year of Publication2013
JournalJournal of medicinal chemistry
Volume56
Issue10
Pages4125-9
Date Published (YYYY/MM/DD)2013/05/23
ISSN Number0022-2623
DOI10.1021/jm400397x
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/23617753?dopt=Abstract