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Azastilbenes: a cut-off to p38 MAPK inhibitors
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Synthetical Organic Chemistry.
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry - BMC, Synthetical Organic Chemistry.
2013 (English)In: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 11, no 27, 4526-4536 p.Article in journal (Refereed) Published
Abstract [en]

Inhibitors with vicinal 4-fluorophenyl/4-pyridine rings on a five- or six-membered heterocyclic ring are known to inhibit the p38 mitogen-activated protein kinase (MAPK), which is a potential target for rheumatoid arthritis and several different types of cancer. Several substituted azastilbene-based compounds with vicinal 4-fluorophenyl/4-pyridine rings were designed using computational docking, synthesized, and evaluated in a cell-free radiometric p38[small alpha] assay. The biochemical evaluation shows that the best inhibition (down to 110 nM) is achieved for azastilbene-based compounds having an isopropylamine substituent in the 2-position of the pyridine ring. The inhibition of p38 signaling in human breast cancer cells was observed for two of the compounds.

Place, publisher, year, edition, pages
2013. Vol. 11, no 27, 4526-4536 p.
National Category
Organic Chemistry
Research subject
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-201387DOI: 10.1039/C3OB27449GISI: 000321601000015OAI: oai:DiVA.org:uu-201387DiVA: diva2:627008
Available from: 2013-06-10 Created: 2013-06-10 Last updated: 2017-12-06Bibliographically approved

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Poon, Jia-FeiDinér, Peter

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