Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.
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 BRAF(V600E) inhibitors. Structure-activity relationship studies of these derivatives revealed that compounds b40 and b47 are the two most potent BRAF(V600E) inhibitors in this series.
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CHEMICAL CHEMICAL GENE-Y GENE-N GENE-Y GENE-N GENE-Y GENE-N GENE-N GENE-N GENE-Y GENE-N
N-(thiophen-2-yl) benzamide N-(thiophen-2-yl) benzamide BRAF kinase BRAF V600E BRAF V600E V600E MAPK BRAF V600E