کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373162 | 981891 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
3,5-Diarylazoles as novel and selective inhibitors of protein kinase D
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The synthesis and preliminary studies of the SAR of novel 3,5-diarylazole inhibitors of Protein Kinase D (PKD) are reported. Notably, optimized compounds in this class have been found to be active in cellular assays of phosphorylation-dependant HDAC5 nuclear export, orally bioavailable, and highly selective versus a panel of additional putative histone deacetylase (HDAC) kinases. Therefore these compounds could provide attractive tools for the further study of PKD / HDAC5 signaling.
The preparation and SAR studies of a novel class of potent selective, and orally bioavailable PKD inhibitors are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1447–1451
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 5, 1 March 2011, Pages 1447–1451
نویسندگان
Gabriel G. Gamber, Erik Meredith, Qingming Zhu, Wanlin Yan, Chang Rao, Michael Capparelli, Robin Burgis, Istvan Enyedy, Ji-Hu Zhang, Nicolas Soldermann, Kimberley Beattie, Olga Rozhitskaya, Keith A. Koch, Nikos Pagratis, Vinayak Hosagrahara,