Zinzalla, G., Haque, M.R., Basu, B Piku, Anderson, J., Kaye, S.L., Haider, S.M., Hasan, F., Antonow, D., Essex, S., Rahman, K.M., Palmer, J., Morgenstern, D., Wilderspin, A.F., Neidle, S. and Thurston, D.E. (2010) A novel small-molecule inhibitor of IL-6 signalling. Bioorganic & Medicinal Chemistry Letters, 20 (23). pp. 7029-32. 10.1016/j.bmcl.2010.09.117.
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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.
|Uncontrolled Keywords:||Small molecule, IL-6 signalling, Inhibitor, STAT3, cancer, inflammation, Interleukin-6, docking|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Cancer Research UK Biomolecular Structure Group|
|Journal or Publication Title:||Bioorganic & Medicinal Chemistry Letters|
|Deposited By:||Library Staff|
|Deposited On:||24 Feb 2011 17:35|
|Last Modified:||11 Nov 2011 16:34|
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