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Issue 27, 2013
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Azastilbenes: a cut-off to p38 MAPK inhibitors

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Abstract

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 p38α 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.

Graphical abstract: Azastilbenes: a cut-off to p38 MAPK inhibitors

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Publication details

The article was received on 18 Dec 2012, accepted on 14 May 2013 and first published on 14 May 2013


Article type: Paper
DOI: 10.1039/C3OB27449G
Citation: Org. Biomol. Chem., 2013,11, 4526-4536
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    Azastilbenes: a cut-off to p38 MAPK inhibitors

    J. Poon, J. P. Alao, P. Sunnerhagen and P. Dinér, Org. Biomol. Chem., 2013, 11, 4526
    DOI: 10.1039/C3OB27449G

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