Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids

IMR OpenIR

	Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids
其他题名	Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids
	Meng Ying 1; Zhang Hongwei 1; Liu Zehua 1; Zeng Shanchao 1; Zhang Hongwei 1; Sun Chiyu 1; Zhang Lijuan 1; Zhao Mingming 1; Wang Guan 2; Jiang Mengying 2; Shi Wei 2; Song Hongrui 1
	2014
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	30 期号:4 页码:624-631
摘要	A series of pyrrolopyrazinone-chalcone hybrids(12a-12q) was designed, synthesized and screened for their antitumor activity against SKOV-3, A549 and HeLa cell lines in vitro. Compared with the pyrrolopyrazinone(10a) and 5-fluorouracil(5-FU), nearly all the tested compounds showed significantly-improved antitumor activities. The most promising compounds 12e and 12k(IC50=0.25 and 0.88 mu mol/L) respectively show activities of 123 and 35 times that of compound 10a(IC50=30.74 mu mol/L) against HeLa cell line. The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.
其他摘要	A series of pyrrolopyrazinone-chalcone hybrids(12a—12q) was designed, synthesized and screened for their antitumor activity against SKOV-3, A549 and HeLa cell lines in vitro. Compared with the pyrrolopyrazi-none(10a) and 5-fluorouracil(5-FU), nearly all the tested compounds showed significantly-improved antitumor activities. The most promising compounds 12e and 12k(IC_(50)=0.25 and 0.88 μmol/L) respectively show activities of 123 and 35 times that of compound 10a(IC_(50)=30.74 μmol/L) against HeLa cell line. The result reveals that the presence of chalcone moiety is beneficial to their activity and selectivity.
关键词	DERIVATIVES CELL HYDROXYCHALCONES AGENTS Pyrrolopyrazinone-chalcone hybrid Antitumor Marine sponge Combination principle
收录类别	CSCD
语种	英语
资助项目	[Program for Liaoning Innovative Research Team in University, China]
CSCD记录号	CSCD:5214900
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/152294
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.吉林大学
推荐引用方式 GB/T 7714	Meng Ying,Zhang Hongwei,Liu Zehua,et al. Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2014,30(4):624-631.
APA	Meng Ying.,Zhang Hongwei.,Liu Zehua.,Zeng Shanchao.,Zhang Hongwei.,...&Song Hongrui.(2014).Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,30(4),624-631.
MLA	Meng Ying,et al."Design, Synthesis and Antitumor Activity of Pyrrolopyrazinone-chalcone Hybrids".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 30.4(2014):624-631.