A novel small-molecule inhibitor of IL-6 signalling.

G. Zinzalla, M.R. Haque, B.P. Basu, J. Anderson, S.L. Kaye, Shozeb Haider, F. Hasan, D. Antonow, S. Essex, K.M. Rahman, J. Palmer, D. Morgenstern, A.F. Wilderspin, S. Neidle, D.E. Thurston

Research output: Contribution to journalArticle

10 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)7029-7032
Number of pages4
JournalBioorganic & Medicinal Chemistry Letters
Volume20(23)
Issue number23
DOIs
Publication statusPublished - 01 Dec 2010

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Fingerprint Dive into the research topics of 'A novel small-molecule inhibitor of IL-6 signalling.'. Together they form a unique fingerprint.

Cite this