کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1355096 1500454 2015 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, thymidine phosphorylase inhibition and molecular modeling studies of 1,3,4-oxadiazole-2-thione derivatives
ترجمه فارسی عنوان
سنتز، مهار تیمیدین فسفرویلاس و مطالعات مدلسازی مولکولی مشتقات 1،3،4-اکسیدازول -2-تیون
کلمات کلیدی
تیمیدین فسفوریلاز، اکسیدیاازول-2-تیون، مدلسازی مولکولی، ضد سرطان
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی


• Efficient synthesis of 1,3,4-oxadiazole-2-thione derivatives.
• Thymidine phosphorylase inhibition studies.
• Molecular docking studies for binding mode investigations.
• Compound 6 bearing 4-hydroxyphenyl group was found to be the most active.

Thymidine phosphorylase (TP) inhibitors have attracted great attention due to their ability to suppress the tumors formation. In our ongoing research, a series of 1,3,4-oxadiazole-2-thione (1–12) has been synthesized under simple reaction conditions in good to excellent yields (86–98%) and their TP inhibition potential has also been evaluated. The majority of synthesized compounds showed moderate thymidine phosphorylase inhibitory activity with IC50 values ranging from 38.24 ± 1.28 to 258.43 ± 0.43 μM, and 7-deazaxanthine (7DX) was used as a reference compound (IC50 38.68 ± 4.42). The TP activity was very much dependent on the C-5 substituents; among this series the compound 6 bearing 4-hydroxyphenyl group was found to be the most active with IC50 38.24 ± 1.28 μM. Molecular docking studies revealed their binding mode.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic Chemistry - Volume 60, June 2015, Pages 37–41
نویسندگان
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