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

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Hayashi Y,Skwarczynski M,Hamada Y,Sohma Y,Kimura T,Kiso Y

doi

10.1021/jm034112n

keywords:

subject

Has Abstract

pub_date

2003-08-28 00:00:00

pages

3782-4

issue

18

eissn

0022-2623

issn

1520-4804

journal_volume

46

pub_type

杂志文章

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