کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5155700 | 1379496 | 2016 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of novel benzo-α-pyrone containing piperazine derivatives as potential BRAFV600E inhibitors
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

چکیده انگلیسی
Virtual screening and scaffold growth were combined together to achieve a series of novel compounds (3a-3n) bearing the benzo-α-pyrone scaffold. Among them, compound 3l showed most powerful antiproliferative activity (IC50 = 2.24 μM for A375 and IC50 = 1.35 μM for WM266-4) and enzyme inhibition activity (IC50 = 0.37 μM). 3l could effectively cause melanoma cells apoptosis in a dose-dependent manner, significantly induce DNA fragmentation and arrest cell cycle at the G0/G1 phase. Docking simulation was performed to explore the binding model of compound 3l with BRAFV600E.74
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 20, 15 October 2016, Pages 4983-4991
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 20, 15 October 2016, Pages 4983-4991
نویسندگان
Long-Wang Chen, Ze-Feng Wang, Bo Zhu, Ruo-Jun Man, Yan-Dong Liu, Yuan-Heng Zhang, Bao-Zhong Wang, Zhong-Chang Wang, Hai-Liang Zhu,