Synthesis and Biological Evaluation of a Series of Novel Celastrol Derivatives with Amino Acid Chain

文献类型： 外文期刊

第一作者： Pang, Chaohai

作者： Pang, Chaohai;Luo, Jinhui;Liu, Chunhua;Wu, Xuejin;Wang, Dingyong

作者机构：

关键词： celastrol; synthesis; derivatives; amino acid; cytotoxic activities

期刊名称：CHEMISTRY & BIODIVERSITY （ 影响因子：2.408； 五年影响因子：2.351 ）

ISSN： 1612-1872

年卷期： 2018 年 15 卷 5 期

页码：

收录情况： SCI

摘要： The synthesis of celastrol analogues containing amino acid ester at the C(29) position and their evaluation for cytotoxic activities invitro were reported. The MTT test showed that a set of derivatives with lower IC50 values than that of the positive control group cisplatin and the parent compound celastrol, which exhibited greater antiproliferative activities. The most potent title compounds 2a and 2e exhibited cytotoxic activities invitro against HeLa and A549 cell lines with IC50 values of 0.371 and 0.237m, 0.235 and 0.109m, respectively. The apoptosis assay demonstrated that 2a and 2e can induces of A549 cell apoptosis in low concentrations. These results showed that 2a and 2e may be promising for further research as antitumor agents.

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