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

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Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin
15 May 2006
Shudong Wang, , Nikolai Z. Zhelev, Susan Duff and Peter M. Fischer
Bioorganic & Medicinal Chemistry Letters
Abstract
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.
Graphical abstract
Synthesis of paclitaxel?penetratin (pAntp) constructs, in which the 2'- or 7-position of paclitaxel was used as the attachment site for linkers connecting the drug and peptide moieties, is described. Conjugates 3b and 3c were highly soluble and stable with a half-life of >8 h under cell culture conditions. Their antitumour activities were determined.
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