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 | |
| Publication status | Published - May 2006 |
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Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin. / Wang, Shudong; Zhelev, Nikolai; Duff, Susan; Fischer, Peter M.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 16, No. 10, 05.2006, p. 2628-2631.Research output: Contribution to journal › Article
TY - JOUR
T1 - Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin
AU - Wang, Shudong
AU - Zhelev, Nikolai
AU - Duff, Susan
AU - Fischer, Peter M.
PY - 2006/5
Y1 - 2006/5
N2 - 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.
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
M3 - Article
VL - 16
SP - 2628
EP - 2631
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 10
ER -