A novel small-molecule inhibitor of IL-6 signalling was written by Zinzalla, Giovanna;Haque, Mohammad R.;Piku Basu, B.;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.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Formula: C4H6N2S This article mentions the following:
A small library of pyrrolidinesulfonylaryl mols., e.g. I, has been synthesized via an efficient 4-step route, and members evaluated for their ability to inhibit IL-6 signalling. One mol., I, was found to have promising activity against IL-6/STAT3 (interleukin-6/signal transducer and activator of transcription-3) 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) vs. A4 (STAT3-null) cells suggesting STAT3-specific inhibitory properties. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Formula: C4H6N2S).
Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Formula: C4H6N2S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica