کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10585775 981378 2013 16 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, biological and structural evaluation of functionalized resveratrol analogues as inhibitors of quinone reductase 2
ترجمه فارسی عنوان
طراحی، سنتز، ارزیابی بیولوژیکی و ساختاری آنالوگهای رزوراترول کاربردی به عنوان مهارکننده های کینون ردوکتاز 2
کلمات کلیدی
کوئینرون ردوکتاز 2، رزوراترول، مهار کننده ها، کتابخانه، کریستالوگرافی اشعه ایکس، سنتز آلی،
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
Resveratrol (3,5,4′-trihydroxylstilbene) has been proposed to elicit a variety of positive health effects including protection against cancer and cardiovascular disease. The highest affinity target of resveratrol identified so far is the oxidoreductase enzyme quinone reductase 2 (QR2), which is believed to function in metabolic reduction and detoxification processes; however, evidence exists linking QR2 to the metabolic activation of quinones, which can lead to cell toxicity. Therefore, inhibition of QR2 by resveratrol may protect cells against reactive intermediates and eventually cancer. With the aim of identifying novel inhibitors of QR2, we designed, synthesized, and tested two generations of resveratrol analogue libraries for inhibition of QR2. In addition, X-ray crystal structures of six of the resveratrol analogues in the active site of QR2 were determined. Several novel inhibitors of QR2 were successfully identified as well as a compound that inhibits QR2 with a novel binding orientation.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 19, 1 October 2013, Pages 6022-6037
نویسندگان
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