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

ABSTRACT: 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.

SUBMITTER: Huang B

PROVIDER: S-EPMC3331967 | biostudies-literature | 2012 May

REPOSITORIES: biostudies-literature

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

Huang Baohua B Kukowska-Latallo Jolanta F JF Tang Shengzhuang S Zong Hong H Johnson Kali B KB Desai Ankur A Gordon Chris L CL Leroueil Pascale R PR Baker James R JR

Bioorganic & medicinal chemistry letters 20120321 9

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 platfor ...[more]

PMID: 22480432

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