1558049-60-7Relevant academic research and scientific papers
Podophyllotoxin sugar glucoside and acidylated sugar glucoside and its pharmaceutical compositions and methods for their preparation and use
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Paragraph 0055-0058; 0099-0101, (2016/10/27)
The invention discloses podophyllotoxin glycoside and acylated glycoside shown in a general formula (I). Podophyllotoxin is used as a lead compound, and the 4-locus hydroxyl and 4'-locus methoxyl of the podophyllotoxin are structurally modified to synthes
Synthesis and anticancer activity of glucosylated podophyllotoxin derivatives linked via 4β-triazole rings
Zi, Cheng-Ting,Xu, Feng-Qing,Li, Gen-Tao,Li, Yan,Ding, Zhong-Tao,Zhou, Jun,Jiang, Zi-Hua,Hu, Jiang-Miao
, p. 13992 - 14012 (2014/01/06)
A series of 4β-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 μM, 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.
