< Back to Publications
Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction in β-Cells with Improved Aqueous Solubility.
|Publication Type||Journal Article|
|Authors||Scully, SS, Tang AJ, Lundh M., Mosher CM, Perkins KM, and Wagner BK|
|Abstract||We 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 Publication||2013|
|Journal||Journal of medicinal chemistry|
|Date Published (YYYY/MM/DD)||2013/05/23|