کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361727 981470 2011 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors
چکیده انگلیسی

We recently described several highly potent, triazine (1) and triazolopyrimidine (2) scaffold-based, dual PI3K/mTOR-inhibitors (e.g., 1, PKI-587) that were efficacious in both in vitro and in vivo models. In order to further optimize these compounds we devised a novel series, the 2-oxatriazines, which also exhibited excellent potency and good metabolic stability. Some 2-oxatriazines showed promising in vivo biomarker suppression and induced apoptosis in the MDA-MB-361 breast cancer xenograft model.

Identification of novel 2-oxatriazines as highly potent pan PI3K/mTOR dual inhibitors and their investigation as potential back up candidates to the clinical compound PKI-587.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4773–4778
نویسندگان
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