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积雪草苷衍生物作为生存素抑制剂的合成及抗肿瘤活性评价

Synthesis and antitumor activity evaluation of asiatic acid derivatives as survivin inhibitor.

作者信息

Meng Yan-Qiu, Cui Hua-Bo, Li Lei, Zhang Wei-Chen, Pan Hong-Shuang, Yu Ting-Ting, Li Wei

机构信息

a Department of Pharmaceutical Engineering , Shenyang University of Chemical Technology , Shenyang 110142 , China.

b ShanDong Sito Bio-Technology Co., Ltd. Shenyang Branch , Shenyang 110169 , China.

出版信息

J Asian Nat Prod Res. 2018 Sep;20(9):897-908. doi: 10.1080/10286020.2017.1405940. Epub 2018 Jan 5.

DOI:10.1080/10286020.2017.1405940
PMID:29304559
Abstract

A series of asiatic acid derivatives were synthesized and their cytotoxicities in vitro against two cancer cell lines (HepG2 and SGC7901) were evaluated by MTT assay. The results showed that compounds I, I, and II have more potent anticancer activity than that of the positive control drug paclitaxel. The interactions between the compounds I, I, and II and survivin were also studied by docking simulations.

摘要

合成了一系列齐墩果酸衍生物,并通过MTT法评估了它们对两种癌细胞系(HepG2和SGC7901)的体外细胞毒性。结果表明,化合物I、I和II具有比阳性对照药物紫杉醇更强的抗癌活性。还通过对接模拟研究了化合物I、I和II与生存素之间的相互作用。

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引用本文的文献

1
Pharmacological Properties, Molecular Mechanisms, and Pharmaceutical Development of Asiatic Acid: A Pentacyclic Triterpenoid of Therapeutic Promise.齐墩果酸的药理特性、分子机制及药物开发:一种具有治疗前景的五环三萜类化合物
Front Pharmacol. 2018 Sep 4;9:892. doi: 10.3389/fphar.2018.00892. eCollection 2018.