کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369532 981781 2016 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis of new diarylamides with pyrimidinyl pyridine scaffold and evaluation of their anti-proliferative effect on cancer cell lines
ترجمه فارسی عنوان
سنتز diarylamides جدید با داربست pyrimidinyl پیریدین و ارزیابی اثر ضدتکثیری آنها در رده های سلولی سرطان
کلمات کلیدی
سنتز؛ اثر ضد تکثیری؛ پیریدین Pyrimidinyl؛ Diarylamide؛ ملانوم
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

A new series of diarylamides, having a pyrimidinyl pyridine scaffold, was designed and synthesized. The target compounds were synthesized in three steps. A selected group from the target compounds was tested over a panel of 60 cancer cell lines at a single dose concentration of 10 μM, and the most active compound, 5j, was further tested in a five-dose testing mode to determine its IC50 value over the 60 cell lines. In single-dose testing mode, compound 5j showed the highest growth inhibition against the NCI-60 cancer cell lines, while other tested compounds showed a weak to moderate inhibitory activity against a range of different cancer cell lines. In five-dose testing mode, compound 5j showed strong inhibitory activity in micro molar range against many cancer cell lines. Its major activity was against melanoma cancer cell lines. Therefore, compound 5j is a promising hit compound targeting this severe form of cancer.

Most active compound (5j); IC50 <2.0 μM against 19 cell lines.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 4, 15 February 2016, Pages 1301–1304
نویسندگان
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