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. © 2010 Elsevier Ltd. All rights reserved.
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Zinzalla, G., Haque, M. R., Piku Basu, B., Anderson, J., Kaye, S. L., Haider, S., … Thurston, D. E. (2010). A novel small-molecule inhibitor of IL-6 signalling. Bioorganic and Medicinal Chemistry Letters, 20(23), 7029–7032. https://doi.org/10.1016/j.bmcl.2010.09.117
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