Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
We previously reported the discovery of BRD0476 (1), a small molecule generated by diversity-oriented synthesis that suppresses cytokine-induced ß-cell apoptosis. Herein, we report the synthesis and biological evaluation of 1 and analogs with improved aqueous solubility. By replacing naphthyl with quinoline moieties, we prepared active analogs with up to a 1400-fold increase in solubility from 1. In addition, we demonstrated that compound 1 and analogs inhibit STAT1 signal transduction induced by IFN-¿.
Originalsprog | Engelsk |
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Tidsskrift | Journal of Medicinal Chemistry |
Vol/bind | 56 |
Udgave nummer | 10 |
Sider (fra-til) | 4125-4129 |
Antal sider | 6 |
ISSN | 0022-2623 |
DOI | |
Status | Udgivet - 25 apr. 2013 |
ID: 45424403