کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371695 | 981851 | 2012 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors Design and evaluation of a series of pyrazolopyrimidines as p70S6K inhibitors](/preview/png/1371695.png)
چکیده انگلیسی
The 70-kDa ribosomal protein S6 kinase (p70S6K) is part of the PI3K/AKT/mTOR pathway and has been implicated in cancer. High throughput screening versus p70S6K led to the identification of aminopyrimidine 3a as active inhibitor. Lead optimization of 3a resulted in highly potent, selective, and orally bioavailable pyrazolopyrimidines. In this manuscript we report the structure–activity relationship of this series and pharmacokinetic, pharmacodynamic, and efficacy data of the lead compound 13c.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 6, 15 March 2012, Pages 2283–2286
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 6, 15 March 2012, Pages 2283–2286
نویسندگان
Joerg Bussenius, Neel K. Anand, Charles M. Blazey, Owen J. Bowles, Lynne Canne Bannen, Diva S.-M. Chan, Baili Chen, Erick W. Co, Simona Costanzo, Steven C. DeFina, Larisa Dubenko, Stefan Engst, Maurizio Franzini, Ping Huang, Vasu Jammalamadaka,