Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility
Research output: Contribution to journal › Journal article › Research › peer-review
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-¿.
Original language | English |
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Journal | Journal of Medicinal Chemistry |
Volume | 56 |
Issue number | 10 |
Pages (from-to) | 4125-4129 |
Number of pages | 6 |
ISSN | 0022-2623 |
DOIs | |
Publication status | Published - 25 Apr 2013 |
ID: 45424403