Issue 85, 2013
From the journal:

Chemical Communications

Synthetic modification of salinomycin: selective O-acylation and biological evaluation†

Björn Borgström,a   Xiaoli Huang,b   Martin Pošta,a   Cecilia Hegardt,c   Stina Oredssonb  and  Daniel Strand*a  

* Corresponding authors

a Centre for Analysis and Synthesis, Department of Chemistry, Lund University, Box 124, 221 00 Lund, Sweden
E-mail: daniel.strand@chem.lu.se
Fax: +46 (0)46 222 82 09
Tel: +46 (0)46 222 81 23

b Department of Biology, Lund University, Sweden

c Department of Oncology, Clinical Sciences, Lund University, Sweden

Abstract

Salinomycin has found renewed interest as an agent for prevention of cancer recurrence through selectively targeting cancer stem cells. Strategies for generation of improved salinomycin analogs by individual modification of its hydroxyl groups are presented. An evaluation of the dose–response effects of the resulting library on breast cancer cell lines shows that acylation of the C20 hydroxyl can be used to improve IC50 values down to one fifth that of salinomycin.

Graphical abstract: Synthetic modification of salinomycin: selective O-acylation and biological evaluation

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Article information

DOI
https://doi.org/10.1039/C3CC45983G
Article type
Communication
Submitted
05 Aug 2013
Accepted
21 Aug 2013
First published
03 Sep 2013
This article is Open Access
Creative Commons BY license

Chem. Commun., 2013,49, 9944-9946

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Synthetic modification of salinomycin: selective O-acylation and biological evaluation

B. Borgström, X. Huang, M. Pošta, C. Hegardt, S. Oredsson and D. Strand, Chem. Commun., 2013, 49, 9944 DOI: 10.1039/C3CC45983G

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