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

Shudong Wang (Lead / Corresponding author), Nikolai Z. Zhelev, Susan Duff, Peter M. Fischer

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)2628-2631
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number10
Early online date2 Mar 2006
DOIs
Publication statusPublished - 15 May 2006

Keywords

  • Antitumour activity
  • Cell delivery vector
  • Drug-peptide conjugate
  • Paclitaxel
  • Penetratin

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