4.5 Article

Synthesis of Dendrimer Conjugates with Naproxen and their Anticancer Activity

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CURRENT ORGANIC CHEMISTRY
卷 27, 期 6, 页码 540-545

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BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1385272827666230605160243

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Dendrimers; anticancer activity; conjugates; naproxen; triethylene glycol; esterification reactions

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This study reported the easy synthesis of dendrimer conjugates with four and eight naproxen moieties at the periphery. The cytotoxicity of these dendrimer conjugates was compared to that of dendron-naproxen conjugates. The results showed that dendron conjugates were less toxic than dendrimer conjugates, but dendrimer conjugates exhibited higher cytotoxicity and selectivity against K-562 and SKLU-1.
Here we report the easy synthesis of dendrimer conjugates with four and eight naproxen moieties at the periphery. The synthesis involved two steps protection-deprotection sequence joined with triethylene glycol. A comparison was made between the cytotoxicity of dendron-naproxen conjugates and that of G1.0 G2.0 dendrimer-naproxen conjugates. Cytotoxicity studies showed that dendron conjugates were toxic towards all cancer cell lines studied, and their toxicity was significantly lower than that of dendrimer conjugates. However, dendrimer conjugates showed higher cytotoxicity and selectivity against K-562 and SKLU-1 than dendron conjugates.

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