Synthesis of a Reactive Oxygen Species-Responsive Doxorubicin Derivative

被引：6

作者：

Delehanty, James B. ^{[1
]}

Das, Shivani ^{[1
]}

Goldberg, Efram ^{[2
]}

Sangtani, Ajmeeta ^{[1
]}

Knight, D. Andrew ^{[2
]}

机构：

[1] Naval Res Lab, Ctr Biomol Sci & Engn, Code 6900, Washington, DC 20375 USA

[2] Florida Inst Technol, Chem Dept, 150 West Univ Blvd, Melbourne, FL 32901 USA

来源：

MOLECULES | 2018年 / 23卷 / 07期

关键词：

doxorubicin; heterobifunctional; linker;

D O I：

10.3390/molecules23071809

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A heterobifunctional reactive oxygen species (ROS)-responsive linker for directed drug assembly onto and delivery from a quantum dot (QD) nanoparticle carrier was synthesized and coupled to doxorubicin using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride (EDC)/sulfo-NHS coupling. The doxorubicin conjugate was characterized using H-1 NMR and LC-MS and subsequently reacted under conditions of ROS formation (Cu2+/H2O2) resulting in successful and rapid thioacetal oxidative cleavage, which was monitored using H-1 NMR.

引用

页数：5

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