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 ;
Close
unknown
Tang, Alicia J ;
Close
unknown
Lundh, Morten ;
Close
Section of Endocrinology Research, Department of Biomedical Sciences, Faculty of Health and Medical Sciences, Københavns Universitet
Mosher, Carrie M ;
Close
unknown
Perkins, Kedar M ;
Close
unknown
Wagner, Bridget K
Close
unknown

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

Full text access

On-site access

At institution

Metrics

Example	Finds records
water{}	containing the word "water".
water supplies"{}"	containing the phrase "water supplies".
author:"Doe, John"author:"{}"	containing the prase "Doe, John" in the author field.
title:IEEEtitle:{}	containing the word "IEEE" in the title field.
Need more help?	Advanced search tutorial