کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361491 | 981465 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel selective inhibitors for EGFR-T790M/L858R
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Through a receptor-based and ligand-based combined virtual screening protocol, 21 novel compounds covering 15 scaffolds were identified as novel inhibitors for EGFR-T790M/L858R, among which, 12 of them were identified as selective inhibitors for EGFR-T790M/L858R to wild-type EGFR, and 5 of them exhibited ‘dual-effective’ to wild-type and mutant EGFR. Meanwhile, their antiproliferative effects toward EGFR high-expressing human lung cancer cell (A549), epidermoid carcinoma cell (A431), and the mutant EGFR-dependent cell (NCI-H1975) were also evaluated.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 3, 1 February 2012, Pages 1365–1370
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 3, 1 February 2012, Pages 1365–1370
نویسندگان
Fang Bai, Hongyan Liu, Linjiang Tong, Wei Zhou, Li Liu, Zhenjiang Zhao, Xiaofeng Liu, Hualiang Jiang, Xicheng Wang, Hua Xie, Honglin Li,