| Synthesis and Anticancer Activity of Glucosylated Podophyllotoxin Derivatives Linked via 4 beta-Triazole Rings | |
Zi, Cheng-Ting1,2; Xu, Feng-Qing1; Li, Gen-Tao1; Li, Yan1 ; Ding, Zhong-Tao2; Zhou, Jun1; Jiang, Zi-Hua3; Hu, Jiang-Miao1
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| 2013-11-01 | |
| 发表期刊 | MOLECULES
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| 卷号 | 18期号:11页码:13992-14012 |
| 摘要 | A series of 4 beta-triazole-linked glucose podophyllotoxin conjugates have been designed and synthesized by employing a click chemistry approach. All the compounds were evaluated for their anticancer activity against a panel of five human cancer cell lines (HL-60, SMMC-7721, A-549, MCF-7, SW480) using MTT assays. Most of these triazole derivatives have good anticancer activity. Among them, compound 35 showed the highest potency against all five cancer cell lines tested, with IC50 values ranging from 0.59 to 2.90 mu M, which is significantly more active than the drug etoposide currently in clinical use. Structure-activity relationship analysis reveals that the acyl substitution on the glucose residue, the length of oligoethylene glycol linker, and the 4'-demethylation of podophyllotoxin scaffold can significantly affect the potency of the anticancer activity. Most notably, derivatives with a perbutyrylated glucose residue show much higher activity than their counterparts with either a free glucose or a peracetylated glucose residue. |
| 关键词 | Podophyllotoxin 4 Beta-triazole Ring Click Chemistry Anticancer Activity |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000330311500058 |
| 引用统计 | |
| 文献类型 | 期刊论文 |
| 条目标识符 | http://ir.kib.ac.cn/handle/151853/19221 |
| 专题 | 植物化学与西部植物资源持续利用国家重点实验室 |
| 作者单位 | 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Peoples R China 2.Yunnan Univ, Key Lab Med Chem Nat Resource, Kunming 650091, Peoples R China 3.Lakehead Univ, Dept Chem, Thunder Bay, ON P7B 5E1, Canada |
| 推荐引用方式 GB/T 7714 | Zi, Cheng-Ting,Xu, Feng-Qing,Li, Gen-Tao,et al. Synthesis and Anticancer Activity of Glucosylated Podophyllotoxin Derivatives Linked via 4 beta-Triazole Rings[J]. MOLECULES,2013,18(11):13992-14012. |
| APA | Zi, Cheng-Ting.,Xu, Feng-Qing.,Li, Gen-Tao.,Li, Yan.,Ding, Zhong-Tao.,...&Hu, Jiang-Miao.(2013).Synthesis and Anticancer Activity of Glucosylated Podophyllotoxin Derivatives Linked via 4 beta-Triazole Rings.MOLECULES,18(11),13992-14012. |
| MLA | Zi, Cheng-Ting,et al."Synthesis and Anticancer Activity of Glucosylated Podophyllotoxin Derivatives Linked via 4 beta-Triazole Rings".MOLECULES 18.11(2013):13992-14012. |
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