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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DOI: 10.1016/j.bmcl.2010.09.117
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.
| Item Type: | Article |
|---|---|
| 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 |
| ID Code: | 1782 |
| 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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