| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362548 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
A small library of pyrrolidinesulphonylaryl molecules has been synthesized via an efficient 4-step route, and members evaluated for their ability to inhibit IL-6 signalling. One molecule (6a) was found to have promising activity against IL-6/STAT3 signalling at the low micromolar level, and to selectively inhibit phosphorylation of STAT3 (but not STAT1) in IL-6 stimulated MDA-MB-231 breast cancer and HeLa cell lines. It was also selectively cytostatic in MDA-MB-231 (STAT3-dependent) versus A4 (STAT3-null) cells suggesting STAT3-specific inhibitory properties.
Graphical abstractCompound 6a is a selective inhibitor of the IL-6/STAT3 signalling pathway.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Giovanna Zinzalla, Mohammad R. Haque, B. Piku Basu, John Anderson, Samantha L. Kaye, Shozeb Haider, Fyeza Hasan, Dyeison Antonow, Samantha Essex, Khondaker M. Rahman, Jonathan Palmer, Daniel Morgenstern, Andrew F. Wilderspin, Stephen Neidle,