Synthesis, biological evaluation and molecular docking studies of 3-(1, 3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity

X Li, JL Liu, XH Yang, X Lu, TT Zhao, HB Gong…

文献索引：Li, Xi; Liu, Jia-Lin; Yang, Xian-Hui; Lu, Xiang; Zhao, Ting-Ting; Gong, Hai-Bin; Zhu, Hai-Liang Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 14 p. 4430 - 4436

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被引用次数: 12

摘要

In present study, a series of 3-(1, 3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives (5a–8d) were designed, synthesized, and evaluated for HDAC inhibition and tumor cell antiproliferation. All of these compounds are reported for the first time, the chemical structures of these compounds were confirmed by means of 1H NMR, ESI-MS and elemental analyzes. Among the compounds, compound 8c showed the most potent ...