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A series of novel N-(5-phenyl-1H-pyrazol-3-yl)benzenesulfonamide derivatives (5a–5l) were synthesized and developed as potential BRAFV600E inhibitors. Among them, compound 5l exhibited the most potent inhibitory activity with an IC50 value of… Click to show full abstract
A series of novel N-(5-phenyl-1H-pyrazol-3-yl)benzenesulfonamide derivatives (5a–5l) were synthesized and developed as potential BRAFV600E inhibitors. Among them, compound 5l exhibited the most potent inhibitory activity with an IC50 value of 0.18 μM for BRAFV600E. Antiproliferative assay results indicated that compound 5l have higher antiproliferative activity against WM266.4 and A375 in vitro with IC50 value of 1.58 and 2.04 μM, respectively, which were comparable with the positive control vemurafenib. Molecular docking of 5l into the BRAFV600E active site was performed to determine the probable binding mode.
Journal Title: Medicinal Chemistry Research
Year Published: 2017
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