کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378915 | 982014 | 2005 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
EB1627: a soluble prodrug of the potent anticancer cyanoguanidine CHS828
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
To overcome pharmacokinetic and solubility problems observed in early clinical trials with the potent anticancer compound CHS828, we synthesised a series of prodrugs with improved properties. The best compound obtained was EB1627, with a tetraethyleneglycol moiety attached to the parent drug via a carbonate linkage. This compound was found soluble enough to be given i.v. and the drug was rapidly released in vivo exerting a very potent inhibitory activity alone and in combination with known cytostatics (etoposide) in animal models in vivo.
The preparation and biological activity of (EB1627), a soluble pro-drug of the potent of anticancer cyanoguanidine CHS828, is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 10, 16 May 2005, Pages 2491–2494
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 10, 16 May 2005, Pages 2491–2494
نویسندگان
Ernst Binderup, Fredrik Björkling, Pernille Vig Hjarnaa, Scilla Latini, Bodil Baltzer, Morten Carlsen, Lise Binderup,