کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1257179 971549 2013 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and screen of cathepsin K inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی (عمومی)
پیش نمایش صفحه اول مقاله
Design, synthesis, and screen of cathepsin K inhibitors
چکیده انگلیسی

We synthesized a series of epoxysuccinic acid derivatives and evaluated their in vitro cathepsin K inhibitory activity The screening results show that the potency of compounds 9e, 9d, 9p, 9j and 9k (IC50 ≤ 0.005 μmol/L) were equal to or greater than that of the lead compound 9a. Less hydrophobic compounds showed weaker potency, which can be explained by the hydrophobic nature of the cathepsin K binding pockets.

We synthesized a series of epoxysuccinic acid derivatives and evaluated their in vitro cathepsin K inhibitory activity. The screeningresults show that the potency of compounds 9e, 9d, 9p, 9j and 9k (IC50 ≤ 0.005 μmol/L) were equal to or greater than that of the lead compound 9a.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chinese Chemical Letters - Volume 24, Issue 8, August 2013, Pages 715–718
نویسندگان
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