Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma

doi:10.1007/s00044-022-02890-2

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	Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma
	Sun, Jin-Jin; Wang, Jin-Ping; Li, Tian-Ze; Ma, Yun-Bao; Xue, Dong; Chen, Ji-Jun
	2022
发表期刊	MEDICINAL CHEMISTRY RESEARCH
卷号	31 期号:7 页码:1224-1239
摘要	Our previous study demonstrated that guaiane-type sesquiterpenoid ludartin showed potent antihepatoma activity against two human hepatocellular carcinoma cell lines, HepG2 and Huh7, with IC50 values of 32.7 and 34.3 mu M, respectively. In this study, 34 ludartin derivatives were designed, synthesized and evaluated for their cytotoxic activities against HepG2 and Huh7 cell lines using an MTT assay in vitro. As a result, 17 compounds increased the activity against HepG2 cells, and 20 compounds enhanced the activity against Huh7 cells; 14 derivatives 2, 4-7, 9, 11, 17, 24, 28-30 and 32-33 were superior to ludartin on both HepG2 and Huh7 cells. In particular, dimeric derivative 33 as the most active compound showed 20-fold and 17-fold enhancement of cytotoxicity against HepG2 and Huh7 cells compared to that of ludartin. These results suggested that compound 33 could serve as a promising lead compound against liver cancer. [GRAPHICS] .
关键词	Ludartin derivatives Antihepatoma activity HepG2 cells Huh7 cells SESQUITERPENE LACTONES CHEMICAL-CONSTITUENTS GUAIANOLIDES ANTITUMOR ANALOGS
DOI	10.1007/s00044-022-02890-2
收录类别	SCI
WOS记录号	WOS:000801056800002
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/74756
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Sun, Jin-Jin,Wang, Jin-Ping,Li, Tian-Ze,et al. Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma[J]. MEDICINAL CHEMISTRY RESEARCH,2022,31(7):1224-1239.
APA	Sun, Jin-Jin,Wang, Jin-Ping,Li, Tian-Ze,Ma, Yun-Bao,Xue, Dong,&Chen, Ji-Jun.(2022).Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma.MEDICINAL CHEMISTRY RESEARCH,31(7),1224-1239.
MLA	Sun, Jin-Jin,et al."Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma".MEDICINAL CHEMISTRY RESEARCH 31.7(2022):1224-1239.

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