Design and synthesis of ludartin derivatives as potential anticancer agents against hepatocellular carcinoma
文献类型：期刊论文
| 作者 | Sun, Jin-Jin; Wang, Jin-Ping; Li, Tian-Ze; Ma, Yun-Bao; Xue, Dong; Chen, Ji-Jun
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| 刊名 | MEDICINAL CHEMISTRY RESEARCH
 |
| 出版日期 | 2022 |
| 卷号 | 31期号:7页码:1224-1239 |
| 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 |
| 英文摘要 | 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] . |
| WOS记录号 | WOS:000801056800002 |
| 源URL | [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. |
入库方式： OAI收割
来源：昆明植物研究所
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