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


ABSTRACT: 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.

SUBMITTER: Ai Y 

PROVIDER: S-EPMC6331168 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

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

Ai Yong Y   Obianom Obinna N ON   Kuser Meredith M   Li Yue Y   Shu Yan Y   Xue Fengtian F  

ACS medicinal chemistry letters 20181203 1


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

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