کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362548 | 981490 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A novel small-molecule inhibitor of IL-6 signalling
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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.
Compound 6a is a selective inhibitor of the IL-6/STAT3 signalling pathway.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7029–7032
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 7029–7032
نویسندگان
Giovanna Zinzalla, 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,