Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAFV600E inhibitors |
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| Authors: | Yunfeng Xie Xianjie Chen Jie Qin Xiangqian Kong Fei Ye Yuren Jiang Hong Liu Hualiang Jiang Ronen Marmorstein Cheng Luo |
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| Institution: | 1. College of Chemistry and Chemical Engineering, Central South University, Changsha 410083, China;2. School of Chemistry and Chemical Engineering, Nanjing National Laboratory of Microstructures, Nanjing University, Nanjing 210093, China;3. The Wistar Institute, Philadelphia, PA 19104, USA;4. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China |
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| Abstract: | The V600E BRAF kinase mutation, which activates the downstream MAPK signaling pathway, commonly occurs in about 8% of all human malignancies and about 50% of all melanomas. In this study, we employed virtual screening and chemical synthesis to identify a series of N-(thiophen-2-yl) benzamide derivatives as potent BRAFV600E inhibitors. Structure–activity relationship studies of these derivatives revealed that compounds b40 and b47 are the two most potent BRAFV600E inhibitors in this series. |
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