Huan Ma, Gang Chen, Tao Wang
Sep 1, 2016
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Influential Citations
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Quality indicators
Journal
Chemical Biology & Drug Design
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.