Dyrager, Christine published the artcileDesign, Synthesis, and Biological Evaluation of Chromone-Based p38 MAP Kinase Inhibitors, Category: chlorides-buliding-blocks, the publication is Journal of Medicinal Chemistry (2011), 54(20), 7427-7431, database is CAplus and MEDLINE.
3-(4-Fluorophenyl)-2-(4-pyridyl)chromone derivatives were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position of the pyridyl moiety gave p38α inhibitors with IC50 in the low nanomolar range. For instance, 3-(4-fluorophenyl)-2-[-2-(isopropylamino)-4-pyridinyl]chromone (I) has IC50 of 17 nm. I and its cyclohexylamino counterpart showed excellent selectivity profiles when tested on a panel of 62 kinases, as well as efficient inhibition of p38 signaling in human breast cancer cells.
Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Category: chlorides-buliding-blocks.
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