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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی (عمومی)
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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
Journal: Chinese Chemical Letters - Volume 24, Issue 8, August 2013, Pages 715–718
نویسندگان
Ying-Ying Yu, Wei Sun, Lei Dong, Hai-Dong Liu, Dan Jiang, Jun-Hai Xiao, Xiao-Hong Yang, Song Li,