کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1364443 981537 2013 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4]triazoles as inhibitors of transforming growth factor β1 type 1 receptor
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4]triazoles as inhibitors of transforming growth factor β1 type 1 receptor
چکیده انگلیسی

A series of 2-pyridinyl-[1,2,4]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 12b showed significant ALK5 inhibition (SBE-Luciferase, 73%; p3TP-Luciferase, 85%) at a concentration of 5 μM that is comparable to that of SB-431542 (SBE-Luciferase, 79%; p3TP-Luciferase, 88%), but weak p38α MAP kinase inhibition (4%) at a concentration of 10 μM that is much lower than that of SB-431542 (54%). The binding mode of 12b generated by flexible docking studies revealed that the structure of 12b is a good fit into the (NPC-30345)-binding cavity of ALK5.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 12, Issue 9, 1 May 2004, Pages 2013–2020
نویسندگان
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