کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361737 | 981470 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors](/preview/png/1361737.png)
چکیده انگلیسی
The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.
This manuscript is related to the identification of a novel series of GSK-3 inhibitors by a computational analysis based on docking experiments and synthesis of a structure based array on of 2-(4-pyridyl)thienopyridinone core. This approach allowed a timely and efficient way to identify initial starting points for future lead optimization efforts.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4823–4827
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4823–4827
نویسندگان
Gabriella Gentile, Giovanni Bernasconi, Alfonso Pozzan, Giancarlo Merlo, Paola Marzorati, Paul Bamborough, Benjamin Bax, Angela Bridges, Caroline Brough, Paul Carter, Geoffrey Cutler, Margarete Neu, Mia Takada,