کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586294 | 981389 | 2013 | 25 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, biological evaluation, and molecular docking studies of novel 1,3,4-oxadiazole derivatives possessing benzotriazole moiety as FAK inhibitors with anticancer activity
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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, biological evaluation, and molecular docking studies of novel 1,3,4-oxadiazole derivatives possessing benzotriazole moiety as FAK inhibitors with anticancer activity Synthesis, biological evaluation, and molecular docking studies of novel 1,3,4-oxadiazole derivatives possessing benzotriazole moiety as FAK inhibitors with anticancer activity](/preview/png/10586294.png)
چکیده انگلیسی
A series of 1,3,4-oxadiazole derivatives have been designed and synthesized, and their biological activities were also evaluated for FAK inhibitory activity. Compound 4 possessed the most potent enzyme inhibition activities (IC50 = 1.2 ± 0.3 μM for FAK) and anticancer activities (IC50 = 5.68 μg/ml for MCF-7 and IC50 = 10.21 μg/ml for HT29). Structure-activity relationship was also analysed to provide more pharmacophore understanding that could be used to design new agents with more potent FAK inhibitory activity. Docking simulation was performed to explore the binding model of compound 4 with FAK.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 13, 1 July 2013, Pages 3723-3729
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 13, 1 July 2013, Pages 3723-3729
نویسندگان
Shuai Zhang, Yin Luo, Liang-Qiang He, Zhi-Jun Liu, Ai-Qin Jiang, Yong-Hua Yang, Hai-Liang Zhu,