کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375028 | 981931 | 2009 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and SAR of C12–C13-oxazoline derivatives of epothilone A
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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 SAR of C12–C13-oxazoline derivatives of epothilone A Synthesis and SAR of C12–C13-oxazoline derivatives of epothilone A](/preview/png/1375028.png)
چکیده انگلیسی
The SAR of a series of new epothilone A derivatives with a 2-substituted-1,3-oxazoline moiety trans-fused to the C12–C13 bond of the deoxy macrocycle have been investigated with regard to tubulin polymerization induction and cancer cell growth inhibition. Significant differences in antiproliferative activity were observed between different analogs, depending on the nature of the substituent at the 2-position of the oxazoline ring. The most potent compounds showed comparable activity with the natural product epothilone A. Modeling studies provide a preliminary rationale for the observed SAR.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 14, 15 July 2009, Pages 3760–3763
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 14, 15 July 2009, Pages 3760–3763
نویسندگان
Bernhard Pfeiffer, Kurt Hauenstein, Philipp Merz, Jürg Gertsch, Karl-Heinz Altmann,