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

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Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility. / Scully, Stephen Shane; Tang, Alicia J; Lundh, Morten; Mosher, Carrie M; Perkins, Kedar M; Wagner, Bridget K.

In: Journal of Medicinal Chemistry, Vol. 56, No. 10, 25.04.2013, p. 4125-4129.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Scully, SS, Tang, AJ, Lundh, M, Mosher, CM, Perkins, KM & Wagner, BK 2013, 'Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility', Journal of Medicinal Chemistry, vol. 56, no. 10, pp. 4125-4129. https://doi.org/10.1021/jm400397x

APA

Scully, S. S., Tang, A. J., Lundh, M., Mosher, C. M., Perkins, K. M., & Wagner, B. K. (2013). Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility. Journal of Medicinal Chemistry, 56(10), 4125-4129. https://doi.org/10.1021/jm400397x

Vancouver

Scully SS, Tang AJ, Lundh M, Mosher CM, Perkins KM, Wagner BK. Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility. Journal of Medicinal Chemistry. 2013 Apr 25;56(10):4125-4129. https://doi.org/10.1021/jm400397x

Author

Scully, Stephen Shane ; Tang, Alicia J ; Lundh, Morten ; Mosher, Carrie M ; Perkins, Kedar M ; Wagner, Bridget K. / Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility. In: Journal of Medicinal Chemistry. 2013 ; Vol. 56, No. 10. pp. 4125-4129.

Bibtex

@article{cc63fa59dc72472384b7b07fac78fe81,
title = "Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In {\ss}-Cells With Improved Aqueous Solubility",
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-¿.",
author = "Scully, {Stephen Shane} and Tang, {Alicia J} and Morten Lundh and Mosher, {Carrie M} and Perkins, {Kedar M} and Wagner, {Bridget K}",
year = "2013",
month = apr,
day = "25",
doi = "10.1021/jm400397x",
language = "English",
volume = "56",
pages = "4125--4129",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "10",

}

RIS

TY - JOUR

T1 - Small-Molecule Inhibitors of Cytokine-Mediated STAT1 Signal Transduction In ß-Cells With Improved Aqueous Solubility

AU - Scully, Stephen Shane

AU - Tang, Alicia J

AU - Lundh, Morten

AU - Mosher, Carrie M

AU - Perkins, Kedar M

AU - Wagner, Bridget K

PY - 2013/4/25

Y1 - 2013/4/25

N2 - 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-¿.

AB - 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-¿.

U2 - 10.1021/jm400397x

DO - 10.1021/jm400397x

M3 - Journal article

C2 - 23617753

VL - 56

SP - 4125

EP - 4129

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 10

ER -

ID: 45424403