کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360793 | 981448 | 2009 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of novel stilbene-based antitumor agents
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of novel stilbene derivatives has been synthesized and studied with the main goal to investigate SAR of the amino compound 1a, as well as to improve its water solubility, a potentially negative aspect of the molecule that could be a serious obstacle for a pre-clinical development. We have obtained derivatives with good cytotoxic activity, in particular, the derivatives 5c and 6b could represent two novel leads for further investigation. Compound 8b, a morpholino-carbamate derivative, prodrug of 1a, has a very good solubility in water, and is active in suppressing growth of tumor cells at a concentration of 5000 nM, which is a concentration 100 times higher than the parent stilbene 1a.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 2, 15 January 2009, Pages 512–522
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 2, 15 January 2009, Pages 512–522
نویسندگان
Daniele Simoni, Francesco Paolo Invidiata, Marco Eleopra, Paolo Marchetti, Riccardo Rondanin, Riccardo Baruchello, Giuseppina Grisolia, Ashutosh Tripathi, Glen E. Kellogg, David Durrant, Ray M. Lee,