Synthesis, Crystallization, and Biological Evaluation of an Orally Active Prodrug of Gemcitabine
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- 作者：David M. Bender ; Jingqi Bao ; Anne H. Dantzig ; William D. Diseroad ; Kevin L. Law ; Nicholas A. Magnus ; Jeffrey A. Peterson ; Everett J. Perkins ; Yangwei J. Pu ; Susan M. Reutzel-Edens ; David M. Remick ; Ja
- 刊名：Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：November 26, 2009
- 年：2009
- 卷：52
- 期：22
- 页码：6958-6961
- 全文大小：707K
- 年卷期：v.52,no.22(November 26, 2009)
- ISSN：1520-4804
文摘
The design, synthesis, and biological characterization of an orally active prodrug (3) of gemcitabine are described. Additionally, the identification of a novel co-crystal solid form of the compound is presented. Valproate amide 3 is orally bioavailable and releases gemcitabine into the systemic circulation after passing through the intestinal mucosa. The compound has entered clinical trials and is being evaluated as a potential new anticancer agent.