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

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

01/12/2010
Resumo

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.
Identificador

http://pure.qub.ac.uk/portal/en/publications/a-novel-smallmolecule-inhibitor-of-il6-signalling(90cdecec-14c2-4071-9c3f-596ef133b1ee).html

http://dx.doi.org/10.1016/j.bmcl.2010.09.117
Idioma(s)

eng
Direitos

info:eu-repo/semantics/restrictedAccess
Fonte

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 , vol 20(23) , no. 23 , pp. 7029-7032 . DOI: 10.1016/j.bmcl.2010.09.117
Palavras-Chave #/dk/atira/pure/subjectarea/asjc/3000/3003 #Pharmaceutical Science #/dk/atira/pure/subjectarea/asjc/3000/3002 #Drug Discovery #/dk/atira/pure/subjectarea/asjc/1600/1605 #Organic Chemistry #/dk/atira/pure/subjectarea/asjc/1300/1313 #Molecular Medicine #/dk/atira/pure/subjectarea/asjc/1300/1312 #Molecular Biology #/dk/atira/pure/subjectarea/asjc/1300/1308 #Clinical Biochemistry #/dk/atira/pure/subjectarea/asjc/1300/1303 #Biochemistry
Tipo

article
Acesso ao item digital