l-Aspartic and l-glutamic acid ester-based ProTides of anticancer nucleosides: Synthesis and antitumoral evaluation

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• 作者：Ling-Jie Gao^a ; Steven De Jonghe^a ; Dirk Daelemans^b ; Piet Herdewijn^a ; ^{piet.herdewijn@kuleuven.be" class="auth_mail" title="E-mail the corresponding author}
• 关键词：ProTides ; Nucleosides ; Prodrugs ; Antitumoral
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 May 2016
• 年：2016
• 卷：26
• 期：9
• 页码：2142-2146
• 全文大小：699 K

文摘

A series of novel aryloxyphosphoramidate nucleoside prodrugs based on l-aspartic acid and l-glutamic acid as amino acid motif has been synthesized and evaluated for antitumoral activity. Depending on the cancer cell line studied and on the nature of the parent nucleoside compound (gemcitabine, 5-iodo-2′-deoxy-uridine, floxuridine or brivudin), the corresponding ProTides are endowed with an improved or decreased cytotoxic activity.