کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373116 | 981890 | 2009 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase](/preview/png/1373116.png)
چکیده انگلیسی
We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.
The discovery and optimization of a novel series of inhibitors of mTOR kinase are described. Compound 31, KU-63794, has low nanomolar potency against mTOR kinase and is highly selective relative to other PI3K-related kinases.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 20, 15 October 2009, Pages 5950–5953
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 20, 15 October 2009, Pages 5950–5953
نویسندگان
Karine Malagu, Heather Duggan, Keith Menear, Marc Hummersone, Sylvie Gomez, Christine Bailey, Peter Edwards, Jan Drzewiecki, Frédéric Leroux, Mar Jimenez Quesada, Gesine Hermann, Stephanie Maine, Carrie-Anne Molyneaux, Armelle Le Gall, James Pullen,