Abstract
A series of 3-methylidene-1H-indol-2(3H)-ones substituted with a 5- or 6-pentafluorosulfanyl group has been synthesized by a Knoevenagel condensation reaction of SF5-substituted oxindoles with a range of aldehydes. The resulting products were characterized by X-ray crystallography studies and were tested for biological activity versus a panel of cell lines and protein kinases. Some exhibited single digit nM activity.
MeSH terms
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Cell Line
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Cell Proliferation / drug effects
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Fluorides / chemical synthesis
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Fluorides / chemistry
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Fluorides / pharmacology*
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry
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Indoles / pharmacology*
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Models, Molecular
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Molecular Structure
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Oxindoles
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Protein Kinases / metabolism*
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Structure-Activity Relationship
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Sulfur Compounds / chemical synthesis
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Sulfur Compounds / chemistry
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Sulfur Compounds / pharmacology*
Substances
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Indoles
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Oxindoles
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Protein Kinase Inhibitors
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Sulfur Compounds
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sulfur pentafluoride cation
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2-oxindole
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Protein Kinases
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Fluorides