کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10592597 | 981796 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction Tetra-substituted imidazoles as a new class of inhibitors of the p53-MDM2 interaction](/preview/png/10592597.png)
چکیده انگلیسی
Capitalizing on crystal structure information obtained from a previous effort in the search for non peptide inhibitors of the p53-MDM2 interaction, we have discovered another new class of compounds able to disrupt this protein-protein interaction, an important target in oncology drug research. The new inhibitors, based on a tetra-substituted imidazole scaffold, have been optimized to low nanomolar potency in a biochemical assay following a structure-guided approach. An appropriate strategy has allowed us to translate the high biochemical potency in significant anti-proliferative activity on a p53-dependent MDM2 amplified cell line.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 9, 1 May 2014, Pages 2110-2114
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 9, 1 May 2014, Pages 2110-2114
نویسندگان
Andrea Vaupel, Guido Bold, Alain De Pover, Thérèse Stachyra-Valat, Joanna Hergovich Lisztwan, Joerg Kallen, Keiichi Masuya, Pascal Furet,