کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370065 | 981807 | 2016 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of EBI-907: A highly potent and orally active B-RafV600E inhibitor for the treatment of melanoma and associated cancers
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A novel series of pyrazolo[3,4-c]isoquinoline derivatives was discovered as B-RafV600E inhibitors through scaffold hopping based on a literature lead PLX4720. Further SAR exploration and optimization led to the discovery of potent B-RafV600E inhibitors with good oral bioavailability in rats and dogs. One of the compounds EBI-907 (13g) demonstrated excellent in vivo efficacy in B-RafV600E dependent Colo-205 tumor xenograft models in mouse and is under preclinical studies for the treatment of melanoma and B-RafV600E associated cancers.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 3, 1 February 2016, Pages 819–823
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 3, 1 February 2016, Pages 819–823
نویسندگان
Biao Lu, Hu Cao, Jingsong Cao, Song Huang, Qiyue Hu, Dong Liu, Ru Shen, Xiaodong Shen, Weikang Tao, Hong Wan, Dan Wang, Yinfa Yan, Liuqing Yang, Jiayin Zhang, Lei Zhang, Lianshan Zhang, Minsheng Zhang,