Abstract
The synthesis of a series of conjugated spermine derivatives with benzoxadiazole, phenylxanthene or bodipy fluorophores is described. These fluorescent probes were used to identify the activity of the polyamine transport system (PTS). N(1)-Methylspermine NBD conjugate 5 proved to have the optimal fluorescence characteristics and was used to show a selectivity for PTS-proficient CHO versus PTS-deficient CHO-MG cells. It can therefore be used as a tool for the selection of cells sensitive to cytotoxic compounds vectored through the PTS.
MeSH terms
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Animals
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Biological Transport
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Boron Compounds / chemistry*
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CHO Cells
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Chemistry, Pharmaceutical / methods*
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Cricetinae
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Cricetulus
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Drug Design
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Fluorescent Dyes / chemistry
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Fluorescent Dyes / pharmacology*
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Humans
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Oxadiazoles / chemical synthesis*
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Oxadiazoles / pharmacology
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Polyamines / chemistry
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Rhodamines / chemistry*
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Spermine / analogs & derivatives
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Spermine / chemical synthesis*
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Spermine / chemistry
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Spermine / pharmacology
Substances
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4,4-difluoro-4-bora-3a,4a-diaza-s-indacene
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7-nitrobenzoxadiazole
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Boron Compounds
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Fluorescent Dyes
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Oxadiazoles
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Polyamines
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Rhodamines
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alpha-methylspermine
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4-nitrobenzofurazan
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Spermine