1260364-62-2Relevant articles and documents
A novel small-molecule inhibitor of IL-6 signalling
Zinzalla, Giovanna,Haque, Mohammad R.,Piku Basu,Anderson, John,Kaye, Samantha L.,Haider, Shozeb,Hasan, Fyeza,Antonow, Dyeison,Essex, Samantha,Rahman, Khondaker M.,Palmer, Jonathan,Morgenstern, Daniel,Wilderspin, Andrew F.,Neidle, Stephen,Thurston, David E.
experimental part, p. 7029 - 7032 (2010/12/25)
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.
