کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586306 | 981389 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Natural product hybrid and its superacid synthesized analogues: Dodoneine and its derivatives show selective inhibition of carbonic anhydrase isoforms I, III, XIII and XIV
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The natural product dodoneine (a dihydropyranone phenolic compound), extracted from African mistletoe Agelanthus dodoneifolius, has been investigated as inhibitor of several human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms. By using superacid chemistry, analogues of the lactone phenolic hybrid lead compound have been synthesized and tested as CA inhibitors. Small chemical modifications of the basic scaffold revealed strong changes in the selectivity profile against different CA isoforms. These new compounds selectively inhibited isoforms CA I (KIs in the range of 0.13-0.76 μM), III (KIs in the range of 5.13-10.80 μM), XIII (KIs in the range of 0.34-0.96 μM) and XIV (KIs in the range of 2.44-7.24 μM), and can be considered as new leads, probably acting as non-zinc-binders, similar to other phenols/lactones investigated earlier.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 13, 1 July 2013, Pages 3790-3794
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 13, 1 July 2013, Pages 3790-3794
نویسندگان
Hélène Carreyre, Jean-Marie Coustard, Grégoire Carré, Clarisse Vandebrouck, Jocelyn Bescond, Maurice Ouédraogo, Jérôme Marrot, Daniella Vullo, Claudiu T. Supuran, Sébastien Thibaudeau,