Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors |
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Authors: | Dyrager Christine Möllers Linda Nilsson Kjäll Linda Karlsson Alao John Patrick Dinér Peter Wallner Fredrik K Sunnerhagen Per Grøtli Morten |
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Affiliation: | Department of Chemistry, Medicinal Chemistry, University of Gothenburg, SE-41296 G?teborg, Sweden. |
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Abstract: | 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 IC(50) in the low nanomolar range (e.g., IC(50) = 17 nm). The inhibitors 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. |
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