New active paclitaxel glucuronide derivative with improved water solubility.
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- Published online on: February 1, 1998 https://doi.org/10.3892/ijo.12.2.391
- Pages: 391-395
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Abstract
Poor solubility of paclitaxel constitutes an important limitation to its administration to cancer patients. In order to increase solubility, while preserving cytotoxicity, a new paclitaxel derivative substituted at the 2' position of the side chain was prepared. The first step consisted in the introduction of a glutaryl group at the 2' position by esterification of the free hydroxyl followed by an amidation with 6-amino hexanol previously attached to a glucuronide group. The new water soluble derivative was cytotoxic in vitro against an ovarian teratocarcinoma cell line.