Design, Synthesis, and Biological Evaluation of a Novel Water-soluble Prodrug of Docetaxel with Amino Acid as a Linker

被引：7

作者：

Ma, Huan ^{[1
]}

Chen, Gang ^{[2
]}

Wang, Tao ^{[2
]}

Li, Qingeng ^{[1
]}

Liu, Yan ^{[1
]}

机构：

[1] Chongqing Med Univ, Sch Pharm, Chongqing 400016, Peoples R China

[2] Jiangsu Nhwa Luokang Pharmaceut Corp Ltd, R&D Dept, Xuzhou 221000, Peoples R China

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2016年 / 88卷 / 03期

关键词：

biological evaluation; Prodrug of docetaxel; synthesis; water-soluble; TAXOL;

D O I：

10.1111/cbdd.12762

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis and preliminary evaluation of derivatives of docetaxel with novel amino acid as a linker named as LK-193LK-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.

引用

页码：363 / 369

页数：7

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