Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor
Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor
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DOI：
10.1002/cmdc.201700718
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发表时间：
2018-03-06
期刊：
影响因子：
3.4
通讯作者：
Hess-Stumpp, Holger
中科院分区：
文献类型：
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作者：
Collin, Marie-Pierre;Lobell, Mario;Hess-Stumpp, Holger
Rogaratinib (BAY 1163877) is a highly potent and selective small-molecule pan-fibroblast growth factor receptor (FGFR) inhibitor (FGFR1-4) for oral application currently being investigated in phase1 clinical trials for the treatment of cancer. In this publication, we report its discovery by denovo structure-based design and medicinal chemistry optimization together with its pharmacokinetic profile.
