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- Dyrager, Christine, 1975, et al.
(författare)
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Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors
- 2011
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Ingår i: Journal of Medicinal Chemistry. ; 54, s. 7427-7431
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Tidskriftsartikel (refereegranskat)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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