Abstract
Starting from the interaction of galangin (3,5,7-trihydroxyflavone) with a cytosolic nucleotide-binding domain of P-glycoprotein, a series of flavonol derivatives was synthesized and tested for their binding affinity towards the same target. The 5,7-dihydroxy-4'-iodoflavonol and 5,7-dihydroxy-4'-n-octylflavonol derivatives displayed much higher binding affinities, with respective increases of 6- and 93-fold as compared to galangin.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / chemistry
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
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Binding Sites
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Chalcone / analogs & derivatives
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Chalcone / chemistry
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Chalcone / metabolism
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Drug Resistance, Multiple*
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Flavonoids / chemical synthesis*
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Flavonoids / chemistry
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Flavonoids / metabolism*
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Flavonols
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Fluorescence
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Kaempferols*
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Molecular Structure
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Protein Binding
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Protein Structure, Tertiary
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Quercetin / analogs & derivatives*
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Quercetin / metabolism
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Recombinant Proteins / metabolism
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Thermodynamics
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Tryptophan / chemistry
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Flavonoids
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Flavonols
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Kaempferols
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Recombinant Proteins
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galangin
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Chalcone
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kaempferol
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Tryptophan
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Quercetin