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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology
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Breast Neoplasms
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Cell Line, Tumor
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Chromones / chemical synthesis*
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Chromones / chemistry
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Chromones / pharmacology
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Drug Design
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Drug Screening Assays, Antitumor
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Female
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Humans
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Models, Molecular
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
Substances
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Antineoplastic Agents
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Chromones
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p38 Mitogen-Activated Protein Kinases