Synthesis and biological evaluation of novel N-(5-phenyl-1H-pyrazol-3-yl)benzenesulfonamide derivatives as potential BRAFV600E inhibitors

被引：0
|
作者：
Zhen-Hua Gong
Jian Yao
Jian-Feng Ji
Jun Yang
Tie Xiang
Chang-Kai Zhou
机构：
[1] The First People Hospital of Nantong,Department of Burn and Plastic Surgery
来源：
Medicinal Chemistry Research | 2017年 / 26卷
关键词：
BRAF; inhibitor; Pyrazole; Molecular docking; Antiproliferative;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
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.
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页码：2583 / 2591
页数：8
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