Issue 21, 2013
From the journal:

Chemical Communications

Synthesis of selective inhibitors of sphingosine kinase 1†

Dong Jae Baek,a   Neil MacRitchie,b   Nigel J. Pyne,b   Susan Pyneb  and  Robert Bittman*a  

* Corresponding authors

a Department of Chemistry and Biochemistry, Queens College of the City University of New York, Flushing, New York, USA
E-mail: robert.bittman@qc.cuny.edu
Tel: +1 718-997-3279

b Cell Biology Group, Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow G4 0RE, UK

Abstract

Sphingosine kinase isoform 1 (SK1) inhibitors may serve as therapeutic agents for proliferative diseases, including hypertension. We synthesized a series of sphingosine-based SK1-selective inhibitors, the most potent of which is RB-005 (IC50 = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.

Graphical abstract: Synthesis of selective inhibitors of sphingosine kinase 1

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Article information

DOI
https://doi.org/10.1039/C3CC00181D
Article type
Communication
Submitted
09 Jan 2013
Accepted
24 Jan 2013
First published
28 Jan 2013
This article is Open Access
Creative Commons BY license

Chem. Commun., 2013,49, 2136-2138

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Synthesis of selective inhibitors of sphingosine kinase 1

D. J. Baek, N. MacRitchie, N. J. Pyne, S. Pyne and R. Bittman, Chem. Commun., 2013, 49, 2136 DOI: 10.1039/C3CC00181D

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