کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375547 | 981941 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: Derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: Derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge Synthesis and biological evaluation of cis-locked vinylogous combretastatin-A4 analogues: Derivatives with a cyclopropyl-vinyl or a cyclopropyl-amide bridge](/preview/png/1375547.png)
چکیده انگلیسی
A series of novel combretastatin A4 analogues, in which the cis-olefinic bridge is replaced by a cyclopropyl-vinyl or a cyclopropyl-amide moiety, were synthesized and evaluated for inhibition of tubulin polymerization and antiproliferative activity. The derivative 9a with a (cis,E)-cyclopropyl-vinyl unit is the most promising compound. As expected, molecular docking of 9a has shown that only one of the cis-cyclopropyl enantiomers is a good ligand for tubulin.
Docking of two representative compounds in the colchicine binding site of tubulin is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 5, 1 March 2009, Pages 1318–1322
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 5, 1 March 2009, Pages 1318–1322
نویسندگان
Nancy Ty, Julia Kaffy, Alban Arrault, Sylviane Thoret, Renée Pontikis, Joelle Dubois, Luc Morin-Allory, Jean-Claude Florent,