Citation: Gao Hui, Wan Chunping, Zhu Jiahong, Xia Yingjiao, Zhang Yanjiao, Mao Zewei. Syntheses and Biological Evaluations of N-Alkylpiperazine Substituted Furanyl Chalcone Derivatives[J]. Chemistry, ;2018, 81(1): 77-82. shu

Syntheses and Biological Evaluations of N-Alkylpiperazine Substituted Furanyl Chalcone Derivatives

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College of Pharmaceutical Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500
2.
Central Laboratory, The No. 1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021

Corresponding author: Mao Zewei, maozw@ynutcm.edu.cn
Received Date: 11 July 2017
Accepted Date: 12 September 2017

Figures(1)

In order to find new potent biological agents, twelve 4'-(N-substitued-1-piperazinyl) furanyl chalcone derivatives (3a~3l) are designed and synthesized by the general principle of molecular hybridization. The structures are characterized by ¹H NMR, ¹³C NMR and HRMS. In vitro cytotoxic activities against a panel of human tumor cell lines (Hela, A549 and SGC7901) are tested by the MTT assay, and the anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages are evaluated. The result indicate that the substituents of the NH group of piperazine ring have an obvious influence on biological activities. Especially, compounds 3j and 3k are found to be the potent compounds against Hela and A549, and compounds 3d has inhibitory effect on the generation of NO, which can be taken as lead compounds for further SAR research.
- Furanyl chalcone,
- Synthesis,
- Biological evaluation
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