کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587915 | 981444 | 2013 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Inhibiting NF-κB-inducing kinase (NIK): Discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The discovery, structure-based design, synthesis, and optimization of NIK inhibitors are described. Our work began with an HTS hit, imidazopyridinyl pyrimidinamine 1. We utilized homology modeling and conformational analysis to optimize the indole scaffold leading to the discovery of novel and potent conformationally constrained inhibitors such as compounds 25 and 28. Compounds 25 and 31 were co-crystallized with NIK kinase domain to provide structural insights.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 5, 1 March 2013, Pages 1238-1244
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 5, 1 March 2013, Pages 1238-1244
نویسندگان
Kexue Li, Lawrence R. McGee, Ben Fisher, Athena Sudom, Jinsong Liu, Steven M. Rubenstein, Mohmed K. Anwer, Timothy D. Cushing, Youngsook Shin, Merrill Ayres, Fei Lee, John Eksterowicz, Paul Faulder, Bohdan Waszkowycz, Olga Plotnikova, Ellyn Farrelly,