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Design, Synthesis a...
Design, Synthesis and Biological Evaluation of Chromone-based p38 MAP Kinase Inhibitors
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- Dyrager, Christine (author)
- University of Gothenburg
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- Nilsson Möllers, Linda (author)
- University of Gothenburg
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- Kjäll, Linda Karlsson (author)
- University of Gothenburg
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- Alao, John Patrick (author)
- University of Gothenburg
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- Diner, Peter (author)
- Uppsala universitet,Institutionen för biokemi och organisk kemi
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- Wallner, Fredrik (author)
- University of Gothenburg
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- Sunnerhagen, Per (author)
- University of Gothenburg
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- Grøtli, Morten (author)
- University of Gothenburg
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(creator_code:org_t)
- 2011-09-26
- 2011
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 54:20, s. 7427-7431
- Related links:
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https://doi.org/10.1...
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Abstract
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- A series of 3-(4-fluorophenyl)-2-(4-pyridyl)-chromone derivs. were synthesized and evaluated as p38 MAP kinase inhibitors. Introduction of an amino group in the 2-position of the pyridyl moiety gave p38 inhibitors with IC50 values in the low nanomolar range (e.g. 8a; IC50 = 17 nm). Addnl., the inhibitors (8a and 8e) demonstrate an excellent selectivity profile towards the p38 kinase among other kinases, as well as inhibition (8e) of p38 signaling in human breast cancer cells. [on SciFinder(R)]
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- ref (subject category)
- art (subject category)
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