Abstract
A novel glucose-conjugated paclitaxel 5 was synthesized using succinic acid as linker between 2'-paclitaxel and methyl 2'-glucopyranose. 5 has not only improved the pharmaceutical properties of paclitaxel, such as solubility and stability, but also enhanced the specific target delivery to MCF-7 cells without the cytotoxicity against normal cells. Therefore, the glucose conjugation may be potentially used in the targeted delivery of other drugs into cells via glucose transporters (GLUTs) for cancer therapy.
MeSH terms
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Antineoplastic Agents, Phytogenic / chemical synthesis*
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Antineoplastic Agents, Phytogenic / pharmacology*
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Cell Line, Tumor
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Cell Membrane / drug effects
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Cell Membrane / metabolism
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Chemical Phenomena
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Chemistry, Physical
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Chromatography, High Pressure Liquid
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Glucose Transport Proteins, Facilitative / metabolism
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Humans
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Indicators and Reagents
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Neoplasms / drug therapy*
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Neoplasms / pathology
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Paclitaxel / analogs & derivatives*
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Paclitaxel / chemical synthesis*
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Paclitaxel / pharmacology
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Solubility
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Succinates / chemical synthesis*
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Succinates / pharmacology
Substances
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2'-paclitaxel methyl 2-glucopyranosyl succinate
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Antineoplastic Agents, Phytogenic
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Glucose Transport Proteins, Facilitative
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Indicators and Reagents
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Succinates
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Paclitaxel