1434081-75-0Relevant articles and documents
Small-molecule inhibitors of cytokine-mediated STAT1 signal transduction in β-cells with improved aqueous solubility
Scully, Stephen S.,Tang, Alicia J.,Lundh, Morten,Mosher, Carrie M.,Perkins, Kedar M.,Wagner, Bridget K.
, p. 4125 - 4129 (2013/06/27)
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.