Modification, Biological Evaluation and SAR Studies of Novel 1H-Pyrazol Derivatives Containing N,N-Disubstituted Urea Moiety as Potential Anti-melanoma Agents
文献类型： 外文期刊
作者： Ruan, Ban-Feng 1 ; Lin, Meng-Xue 1 ; Shao, Qin 1 ; Wang, Tian-Hong 1 ; Zhang, Qing 1 ; Dong, Yu-Lu 1 ; Bu, Chao-Nan 1 ; X 1 ;
作者机构： 1.Hefei Univ Technol, Sch Biol & Med Engn, Hefei 230009, Anhui, Peoples R China
2.Anhui Acad Agr Sci, Tobacco Res Inst, Hefei 230031, Anhui, Peoples R China
关键词： melanoma; BRAF; 1H-pyrazole-4-amines; 1H-pyrazole-4-ureas; SAR
期刊名称：CHEMISTRY & BIODIVERSITY （ 影响因子：2.408； 五年影响因子：2.351 ）
ISSN： 1612-1872
年卷期： 2018 年 15 卷 6 期
页码：
收录情况： SCI
摘要： Malignant melanomas are amongst the most aggressive cancers. BRAF Inhibitors have exhibited therapeutic effects against BRAF-mutant melanoma. In continuation of our earlier studies on anti-melanoma agents based on 1H-pyrazole skeleton, two sets of novel compounds that include 1H-pyrazole-4-amines FA1 - FA13 and corresponding urea derivatives FN1 - FN13 have been synthesized and evaluated for their BRAF(V600E) inhibitory and antiproliferation activities. Compound FN10 displayed the most potent biological activity against BRAF(V600E) (IC50 = 0.066 m) and the A375 human melanoma cell line (GI(50) = 0.81 m), which was comparable to the positive control vemurafenib, and more potent than our previously reported 1H-pyrazole-3-amines and their urea derivatives. The results of SAR studies and molecular docking can guide further optimization and may help to improve potency of these pyrazole-based anti-melanoma agents.
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