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  • Poon, Jia-Fei, et al. (author)
  • Azastilbenes : a cut-off to p38 MAPK inhibitors
  • 2013
  • In: Organic and biomolecular chemistry. - 1477-0520 .- 1477-0539. ; 11:27, s. 4526-4536
  • Journal article (peer-reviewed)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 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.
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Type of publication
journal article (1)
Type of content
peer-reviewed (1)
Author/Editor
Dinér, Peter (1)
Sunnerhagen, Per (1)
Alao, John Patrick (1)
Poon, Jia Fei (1)
University
Uppsala University (1)
Language
English (1)
Research subject (UKÄ/SCB)
Natural sciences (1)
Year

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