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- Poon, Jia-Fei, et al.
(författare)
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Azastilbenes : a cut-off to p38 MAPK inhibitors
- 2013
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Ingår i: Organic and biomolecular chemistry. - 1477-0520 .- 1477-0539. ; 11:27, s. 4526-4536
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Tidskriftsartikel (refereegranskat)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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