کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362753 981495 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase
چکیده انگلیسی

Starting from HTS hit 1a, X-ray co-crystallization and molecular modeling were used to design potent and selective inhibitors of PI3-kinase. Bioavailablity in this series was improved through careful modulation of physicochemical properties. Compound 12 displayed in vivo knockdown of PI3K pharmacodynamic markers such as pAKT, pPRAS40, and pS6RP in a PC3 prostate cancer xenograft model.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 20, 15 October 2010, Pages 6048–6051
نویسندگان
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