Synthesis, anticancer activity and cytotoxicity of 7‐O‐β‐D‐galactosyl‐PEG‐epothilone B

The 7‐O‐β‐D‐galactosyl‐PEG‐epothilone B 6 was successfully synthesized by a combined chemical and enzymatic method. Activity tests showed that compound 6 was low in toxicity and had strong anticancer activity

Abstract

Epothilone, the macrolide compound produced by Sorangium cellulosum, has antitumor activity. Its anti‐tumor mechanism is similar to that of paclitaxel, which promotes the polymerization of tubulin and induces apoptosis. Herein, 7‐O‐β‐D‐galactosyl‐PEG‐epothilone B 6 was synthesized. It showed that the toxicity of the synthesized compound was 1/182 of the epothilone B. In addition, compound 6 also had significant anticancer activity under the action of enzyme.

This article is protected by copyright. All rights reserved.

https://ift.tt/2AoRClU