کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587287 | 981426 | 2013 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors
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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 a new series of N-ylides as protein farnesyltransferase inhibitors Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors](/preview/png/10587287.png)
چکیده انگلیسی
A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds possessed in vitro inhibition potencies in the micromolar range. The nature of the substituents on the pyridine and phenyl units proved to be important in determining inhibitory activity and generally, the replacement of the cyanoacrylonitrile function by a cyanoethylacrylate group decreased the biological potential on farnesyltransferase. These results completed our SAR study on this original class of N-ylides.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 21, 1 November 2013, Pages 5887-5892
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 21, 1 November 2013, Pages 5887-5892
نویسندگان
Cristina-Maria Abuhaie, Alina Ghinet, Amaury Farce, Joëlle Dubois, Benoît Rigo, Elena Bîcu,