کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1378855 | 982012 | 2006 | 4 صفحه PDF | دانلود رایگان |

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]-NH23b and paclitaxel–2′-pAntp[52–58]-NH23c 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.
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.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 10, 15 May 2006, Pages 2628–2631