کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375005 | 981929 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel hydroxamates as highly potent tumor necrosis factor-α converting enzyme inhibitors. Part II: Optimization of the S3′ pocket
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of novel hydroxamates as highly potent tumor necrosis factor-α converting enzyme inhibitors. Part II: Optimization of the S3′ pocket Discovery of novel hydroxamates as highly potent tumor necrosis factor-α converting enzyme inhibitors. Part II: Optimization of the S3′ pocket](/preview/png/1375005.png)
چکیده انگلیسی
A series of cyclopropyl hydroxamic acids were prepared. Many of the compounds displayed picomolar affinity for the TACE enzyme while maintaining good to excellent selectivity profiles versus MMP-1, -2, -3, -7, -14, and ADAM-10. X-ray analysis of an inhibitor in the TACE active site indicated that the molecules bound to the enzyme in the S1′–S3′ pocket.
We herein disclose a novel series of cyclopropyl hydroxamates that are potent and selective TACE inhibitors with Ki values in the picomolar range.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 21, 1 November 2008, Pages 5809–5814
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 21, 1 November 2008, Pages 5809–5814
نویسندگان
Robert D. Mazzola Jr., Zhaoning Zhu, Lisa Sinning, Brian McKittrick, Brian Lavey, James Spitler, Joseph Kozlowski, Shih Neng-Yang, Guowei Zhou, Zhuyan Guo, Peter Orth, Vincent Madison, Jing Sun, Daniel Lundell, Xiaoda Niu,