Small-molecule inhibitors of cytokine-mediated STAT1 signal transduction in β-cells with improved aqueous solubility
SS Scully, AJ Tang, M Lundh, CM Mosher… - Journal of medicinal …, 2013 - ACS Publications
Journal of medicinal chemistry, 2013•ACS Publications
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.
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.
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.
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