کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1378855 982012 2006 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and biological activity of conjugates between paclitaxel and the cell delivery vector penetratin
چکیده انگلیسی

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

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 10, 15 May 2006, Pages 2628–2631
نویسندگان
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