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 |
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Pages (from-to) | 2628-2631 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 16 |
Issue number | 10 |
DOIs | |
Publication status | Published - May 2006 |