1446252-28-3Relevant articles and documents
Azastilbenes: A cut-off to p38 MAPK inhibitors
Poon, Jia-Fei,Alao, John Patrick,Sunnerhagen, Per,Dinér, Peter
, p. 4526 - 4536 (2013/08/23)
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. The Royal Society of Chemistry 2013.