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

doi:10.1016/j.bmcl.2010.09.117

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

School of Medicine, Dentistry and Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

21 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 language	English
Pages (from-to)	7029-7032
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	20(23)
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2010.09.117
Publication status	Published - 01 Dec 2010

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

ASJC Scopus subject areas

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

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Zinzalla, G., Haque, M. R., Basu, B. P., Anderson, J., Kaye, S. L., Haider, S., Hasan, F., Antonow, D., Essex, S., Rahman, K. M., Palmer, J., Morgenstern, D., Wilderspin, A. F., Neidle, S., & Thurston, D. E. (2010). A novel small-molecule inhibitor of IL-6 signalling. Bioorganic & Medicinal Chemistry Letters, 20(23)(23), 7029-7032. https://doi.org/10.1016/j.bmcl.2010.09.117

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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.",

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

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AU - Zinzalla, G.

AU - Haque, M.R.

AU - Basu, B.P.

AU - Anderson, J.

AU - Kaye, S.L.

AU - Haider, Shozeb

AU - Hasan, F.

AU - Antonow, D.

AU - Essex, S.

AU - Rahman, K.M.

AU - Palmer, J.

AU - Morgenstern, D.

AU - Wilderspin, A.F.

AU - Neidle, S.

AU - Thurston, D.E.

PY - 2010/12/1

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AB - 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.

U2 - 10.1016/j.bmcl.2010.09.117

DO - 10.1016/j.bmcl.2010.09.117

M3 - Article

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JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 23

ER -

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

Abstract

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ASJC Scopus subject areas

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