کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371927 | 981860 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery and SAR of hydantoin TACE inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We disclose inhibitors of TNF-α converting enzyme (TACE) designed around a hydantoin zinc binding moiety. Crystal structures of inhibitors bound to TACE revealed monodentate coordination of the hydantoin to the zinc. SAR, X-ray, and modeling designs are described. To our knowledge, these are the first reported X-ray structures of TACE with a hydantoin zinc ligand.
A novel series of hydantoin TACE inhibitors is disclosed. The initial design and SAR optimization of the series, as well as accompanying X-ray structural and modeling considerations, are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 6, 15 March 2010, Pages 1877–1880
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 6, 15 March 2010, Pages 1877–1880
نویسندگان
Wensheng Yu, Zhuyan Guo, Peter Orth, Vincent Madison, Lei Chen, Chaoyang Dai, Robert J. Feltz, Vinay M. Girijavallabhan, Seong Heon Kim, Joseph A. Kozlowski, Brian J. Lavey, Dansu Li, Daniel Lundell, Xiaoda Niu, John J. Piwinski, Janeta Popovici-Muller,