Enhanced Tumor Selectivity of 5-Fluorouracil Using a Reactive Oxygen Species-Activated Prodrug Approach

被引：30

作者：

Ai, Yong ^{[1
]}

Obianom, Obinna N. ^{[1
]}

Kuser, Meredith ^{[1
]}

Li, Yue ^{[2
]}

Shu, Yan ^{[1
,3
]}

Xue, Fengtian ^{[1
]}

机构：

[1] Univ Maryland, Sch Pharm, Dept Pharmaceut Sci, Baltimore, MD 21201 USA

[2] Univ Maryland, Dept Chem & Biochem, College Pk, MD 20740 USA

[3] Guangzhou Med Univ, Sch & Hosp Stomatol, Guangzhou 510140, Guangdong, Peoples R China

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2019年 / 10卷 / 01期

基金：

美国国家卫生研究院;

关键词：

5-Fluorouracil; prodrugs; reactive oxygen species; anticancer; AMINOFERROCENE-BASED PRODRUGS; CROSS-LINKING AGENTS; HYDROGEN-PEROXIDE; CANCER-CELLS; OXIDATIVE STRESS; ROS; PHOSPHORYLASE; MECHANISMS; TOXICITY; STRATEGY;

D O I：

10.1021/acsmedchemlett.8b00539

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the design, synthesis, and evaluation of novel 5-fluorouracil (5FU) prodrugs 1a,1b that are efficiently activated by the high level of reactive oxygen species (ROS) in cancer cells. Prodrugs 1a,1b selectively kill cancer cells over normal cells and are well-tolerated in mice. The strategy described herein can extend application of chemotherapeutic drugs.

引用

页码：127 / 131

页数：9

共 41 条

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