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
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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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
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4773–4778
نویسندگان
Christoph M. Dehnhardt, Aranapakam M. Venkatesan, Zecheng Chen, Efren Delos-Santos, Semiramis Ayral-Kaloustian, Natasja Brooijmans, Ker Yu, Irwin Hollander, Larry Feldberg, Judy Lucas, Robert Mallon,