Hayashi Yoshio, Skwarczynski Mariusz, Hamada Yoshio, Sohma Youhei, Kimura Tooru, Kiso Yoshiaki
Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-Ku, Kyoto 607-8412 Japan.
J Med Chem. 2003 Aug 28;46(18):3782-4. doi: 10.1021/jm034112n.
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.
一种新型水溶性紫杉醇前药异紫杉醇2被合成出来，它通过O-N酰基迁移这种简单的pH依赖化学机制实现了更高的水溶性并生成紫杉醇，在水溶性和动力学方面显示出有前景的结果。这种前药是紫杉醇的2'-O-苯甲酰异构体，在转化为紫杉醇的过程中没有额外的功能性助剂释放出来，这在毒理学和医学经济学方面将是一个很大的优势。
