| Literature DB >> 21030257 |
Giovanna Zinzalla1, 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, David E Thurston.
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.Entities:
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Year: 2010 PMID： 21030257 DOI： 10.1016/j.bmcl.2010.09.117
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823