The facile synthesis of multifunctional PAMAM dendrimer conjugates through copper-free click chemistry

被引：32

作者：

Huang, Baohua ^{[1
]}

Kukowska-Latallo, Jolanta F. ^{[1
]}

Tang, Shengzhuang ^{[1
]}

Zong, Hong ^{[1
]}

Johnson, Kali B. ^{[1
]}

Desai, Ankur ^{[1
]}

Gordon, Chris L. ^{[1
]}

Leroueil, Pascale R. ^{[1
]}

Baker, James R., Jr. ^{[1
]}

机构：

[1] Univ Michigan, Michigan Nanotechnol Inst Med & Biol Sci, Ann Arbor, MI 48109 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 09期

基金：

美国国家卫生研究院;

关键词：

PAMAM dendrimer; Copper-free click conjugation; Drug delivery; DRUG-DELIVERY; FUNCTIONALIZATION; GROWTH;

D O I：

10.1016/j.bmcl.2012.03.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The facile conjugation of three azido modified functionalities, namely a therapeutic drug (methotrexate), a targeting moiety (folic acid), and an imaging agent (fluorescein) with a G5 PAMAM dendrimer scaffold with cyclooctyne molecules at the surface through copper-free click chemistry is reported. Mono-, di-, and tri-functional PAMAM dendrimer conjugates can be obtained via combinatorial mixing of different azido modified functionalities simultaneously or sequentially with the dendrimer platform. Preliminary flow cytometry results indicate that the folic acid targeted nanoparticles are efficiently binding with KB cells. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：3152 / 3156

页数：5

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