Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin

Shudong Wang, Nikolai Zhelev, Susan Duff, Peter M. Fischer

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Synthesis of paclitaxel–penetratin (pAntp) constructs, in which the 2′- or 7-position of paclitaxel was used as the attachment site for linker connecting the drug and peptide moieties, is described. Paclitaxel–2′-pAntp[43–58]-NH2 3b and paclitaxel–2′-pAntp[52–58]-NH2 3c showed excellent antitumour activity against human lung and breast cancer cell lines. These conjugates were highly soluble and stable with a half-life of >8 h under cell culture conditions. The drug–peptide conjugates may be therapeutically useful due to improved pharmaceutical properties.

Original languageEnglish
Pages (from-to)2628-2631
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number10
Publication statusPublished - May 2006


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