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

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• 作者：Baohua Huang ; ^{baohua@med.umich.edu} ; ^{baohua@umich.edu} ; Jolanta F. Kukowska-Latallo ; Shengzhuang Tang ; Hong Zong ; Kali B. Johnson ; Ankur Desai ; Chris L. Gordon ; Pascale R. Leroueil ; James R. Baker Jr. ; ^{jbakerjr@med.umich.edu}
• 关键词：PAMAM dendrimer ; Copper-free click conjugation ; Drug delivery
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 May, 2012
• 卷：22
• 期：9
• 页码：3152-3156
• 文件大小：754 K

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.