Abstract
The synthesis and preliminary evaluation of derivatives of docetaxel with novel amino acid as a linker named as LK-193˜LK-196 was described. The C2'-modified compound LK-196 behaves as a prodrug; that is, docetaxel is generated upon exposure to human plasma. The compound was also found to have greatly improved water solubility. The pharmacodynamic results showed LK-196 had the self-evident inhibitory effect on tumor growth in vivo, which is a promising candidate for further biological evaluation.
Keywords:
Prodrug of docetaxel; biological evaluation; synthesis; water-soluble.
© 2016 John Wiley & Sons A/S.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / therapeutic use*
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Cell Line, Tumor
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Cell Survival / drug effects
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Docetaxel
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Drug Design*
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Humans
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Male
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Mice
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Mice, Inbred BALB C
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Mice, Nude
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Neoplasms / drug therapy
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Neoplasms / pathology
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Prodrugs / chemical synthesis
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Prodrugs / chemistry*
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Prodrugs / pharmacokinetics
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Prodrugs / therapeutic use*
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Rats, Sprague-Dawley
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Solubility
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Taxoids / chemical synthesis
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Taxoids / chemistry*
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Taxoids / pharmacokinetics
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Taxoids / therapeutic use*
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Water / chemistry
Substances
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Antineoplastic Agents
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Prodrugs
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Taxoids
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Water
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Docetaxel