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

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

doi:10.1016/j.bmcl.2006.02.035

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

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

Abertay University

Research output: Contribution to journal › Article

14 Citations (Scopus)

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.

Original language	English
Pages (from-to)	2628-2631
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2006.02.035
Publication status	Published - May 2006

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Wang, S., Zhelev, N., Duff, S., & Fischer, P. M. (2006). Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin. Bioorganic and Medicinal Chemistry Letters, 16(10), 2628-2631. https://doi.org/10.1016/j.bmcl.2006.02.035

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AU - Wang, Shudong

AU - Zhelev, Nikolai

AU - Duff, Susan

AU - Fischer, Peter M.

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AB - 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.

U2 - 10.1016/j.bmcl.2006.02.035

DO - 10.1016/j.bmcl.2006.02.035

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