Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives

doi:10.6023/cjoc201707034

Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (3): 684-691.DOI: 10.6023/cjoc201707034 Previous Articles Next Articles

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新型取代查尔酮-哌嗪衍生物的合成及其生物活性评价

高慧^a, 郑喜^b, 朱萍^a, 王斯^a, 万春平^b, 饶高雄^a, 毛泽伟^a

a 云南中医学院中药学院昆明 650500;
b 云南中医学院第一附属医院中心实验室昆明 650021

收稿日期:2017-07-30 修回日期:2017-10-24 发布日期:2017-11-15
通讯作者: 万春平,E-mail:wanchunping1012@163.com;毛泽伟,E-mail:maozw@ynutcm.edu.cn E-mail:wanchunping1012@163.com;maozw@ynutcm.edu.cn
基金资助:
国家自然科学基金（Nos.81560620，81460624）、云南省应用基础研究（No.2014FZ078）和云南省科学技术厅-云南中医学院应用基础研究联合专项[No.2017FF117（-023）]资助项目.

Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives

Gao Hui^a, Zheng Xi^b, Zhu Ping^a, Wang Si^a, Wan Chunping^b, Rao Gaoxiong^a, Mao Zewei^a

a College of Pharmaceutical Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500;
b Central Laboratory, The NO.1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021

Received:2017-07-30 Revised:2017-10-24 Published:2017-11-15
Contact: 10.6023/cjoc201707034 E-mail:wanchunping1012@163.com;maozw@ynutcm.edu.cn
Supported by:
Project supported by the National Natural Science Foundation of China (Nos. 81560620, 81460624), the Application Basic Research Program of Yunnan Province (No. 2014FZ078) and the Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Traditional Chinese Medicine[No. 2017FF117(-023)].

1. Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives.PDF(6323KB)

Abstract

A series of novel substituted chalcone-piperazine derivatives have been synthesized, and screened in vitro anti-inflammatory in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and cytotoxic activity against 3 strains human tumor cell lines. The results demonstrated that the substituents of the core ring and the NH group of piperazine ring had obvious influences on biological activities. Especially, 3,4,5-trimethoxy-4'-[N-(2-oxopropyl)-1-piperazinyl]chalcone (11) showed better inhibitory effect on the generation of NO (IC₅₀=3.81 μmol/L), and 4-bromo-4'-[N-(4'-methyl-2-oxophenylethyl)-1-piperazinyl]chalcone (25) displayed good cytotoxic activity against A549, Hela and sk-ov-3 (IC₅₀=0.54, 0.05 and 9.12 μmol/L, respectively).

Key words: chalcone-piperazine derivatives, anti-inflammatory activity, cytotoxic activity

Cite this article

Gao Hui, Zheng Xi, Zhu Ping, Wang Si, Wan Chunping, Rao Gaoxiong, Mao Zewei. Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives[J]. Chin. J. Org. Chem., 2018, 38(3): 684-691.

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新型取代查尔酮-哌嗪衍生物的合成及其生物活性评价

Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives

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