Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility

Stephen Shane Scully; Alicia J Tang; Morten Lundh; Carrie M Mosher; Kedar M Perkins; Bridget K Wagner

doi:10.1021/jm400397x

Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility

Authors:

Scully, Stephen Shane ;
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Tang, Alicia J ;
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Lundh, Morten ;
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Endocrinology and Metabolism, Department of Biomedical Sciences, Faculty of Health and Medical Sciences, Københavns Universitet
Mosher, Carrie M ;
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Perkins, Kedar M ;
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Wagner, Bridget K
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DOI:

10.1021/jm400397x

Abstract:

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-¿.

Type:

Journal article

Language:

English

Published in:

Journal of Medicinal Chemistry, 2013, Vol 56, Issue 10, p. 4125-4129

Main Research Area:

Medical science

Publication Status:

Published

Review type:

Peer Review

Submission year:

2013

Scientific Level:

Scientific

ID:

241859814

Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility

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