A novel approach of water-soluble paclitaxel prodrug with no auxiliary and no byproduct: Design and synthesis of isotaxel

被引：81

作者：

Hayashi, Y ^{[1
]}

Skwarczynski, M ^{[1
]}

Hamada, Y ^{[1
]}

Sohma, Y ^{[1
]}

Kimura, T ^{[1
]}

Kiso, Y ^{[1
]}

机构：

[1] Kyoto Pharmaceut Univ, Ctr Frontier Res Med Sci, Dept Med Chem, Yamashina Ku, Kyoto 6078412, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 18期

关键词：

D O I：

10.1021/jm034112n

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel water-soluble paclitaxel prodrug, isotaxel 2, that realizes a higher water-solubility and the formation of paclitaxel through a simple pH-dependent chemical mechanism via the O-N acyl migration was synthesized and showed promising results in water-solubility and kinetics. This prodrug, a 2'-O-benzoyl isoform of paclitaxel, has no additional functional auxiliaries released during conversion to paclitaxel, which would be a great advantage in toxicology and medical economics.

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页码：3782 / 3784

页数：3

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