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Design, synthesis, ...
Design, synthesis, and biological evaluation of chromone-based p38 MAP kinase inhibitors
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- Dyrager, Christine, 1975 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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- Möllers, Linda N (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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- Kjäll, Linda K (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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- Alao, John Patrick, 1973 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för cell- och molekylärbiologi,Department of Cell and Molecular Biology
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- Dinér, Peter, 1976 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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- Wallner, Fredrik (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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- Sunnerhagen, Per, 1959 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för cell- och molekylärbiologi,Department of Cell and Molecular Biology
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- Grøtli, Morten, 1966 (author)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi,Department of Chemistry
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(creator_code:org_t)
- 2011
- 2011
- English.
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In: Journal of Medicinal Chemistry. ; 54, s. 7427-7431
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Dyrager, Christi ...
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Möllers, Linda N
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Kjäll, Linda K
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Alao, John Patri ...
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Dinér, Peter, 19 ...
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Wallner, Fredrik
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show more...
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Sunnerhagen, Per ...
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Grøtli, Morten, ...
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Cell and Molecul ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
- Articles in the publication
- Journal of Medic ...
- By the university
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University of Gothenburg