Synthesis of Reactive Polymers for Acrolein Capture Using AGET ATRP

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• 作者：Laura T. Beringer ; Shaohua Li ; Gary Gilmore ; John Lister ; Saadyah Averick
• 刊名：Molecular Pharmaceutics
• 出版年：2015
• 出版时间：October 5, 2015
• 年：2015
• 卷：12
• 期：10
• 页码：3776-3781
• 全文大小：375K
• ISSN：1543-8392

文摘

Acrolein is a toxic metabolite of the anticancer agent cyclophosphamide (CP). Current strategies to mitigate acrolein toxicity are insufficient, and in this brief article, we report the synthesis of well-defined low molecular weight block copolymers using activators generated by electron transfer atom transfer radical polymerization (AGET ATRP) capable of reacting with the cytotoxic small molecule acrolein. Acrolein reactivity was introduced into the block copolymers via incorporation of either (a) aminooxy or (b) sulfhydryl groups. The cytoprotective effect of the polymers was compared to sodium 2-sulfanylethanesulfonate (mesna) the current gold standard for protection from CP urotoxicity, and we found that the polymers bearing sulfhydryl moieties demonstrated superior cytoprotective activity.