H-Gemcitabine: A New Gemcitabine Prodrug for Treating Cancer

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• 作者：Madhuri Dasari ; Abhinav P. Acharya ; Dongin Kim ; Seungjun Lee ; Sungmun Lee ; Jeanne Rhea ; Ross Molinaro ; Niren Murthy
• 刊名：Bioconjugate Chemistry
• 出版年：2013
• 出版时间：January 16, 2013
• 年：2013
• 卷：24
• 期：1
• 页码：4-8
• 全文大小：280K
• 年卷期：v.24,no.1(January 16, 2013)
• ISSN：1520-4812

文摘

In this report, we present a new strategy for targeting chemotherapeutics to tumors, based on targeting extracellular DNA. A gemcitabine prodrug was synthesized, termed H-gemcitabine, which is composed of Hoechst conjugated to gemcitabine. H-gemcitabine has low toxicity because it is membrane-impermeable; however, it still has high tumor efficacy because of its ability to target gemcitabine to E-DNA in tumors. We demonstrate here that H-gemcitabine has a wider therapeutic window than free gemcitabine.