期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 162, 期 -, 页码 122-131出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.10.059
关键词
Fusidic acid; Derivatives; Synthesis; Anti-tumor activity; Apoptosis
资金
- Taishan Scholar Project, NSFC [81773563, 81728020]
- Key Research Project of Shandong Province [2017GSF18177]
- Natural Science Foundation of Shandong Province [ZR2018LH025]
A series of novel fusidic acid (FA) derivatives were synthesized and screened for their in vitro cytotoxicity against the Hela, U87, KBV and MKN45 cancer cell lines. Selected FA derivatives with anti-tumor activity were firstly identified including compound 4, which exhibited good anti-proliferative activity with IC50 values in the range of 1.26-3.57 mu M. Further research revealed that compound 4 induced Hela cells to undergo apoptosis by increasing the ratio of the cells in the Sub-G(0)/G(1) phase via decreasing the neo-synthesized proteins in a dose-dependent manner from 1 to 10 mu M. Compound 4 also showed good in vivo anti-tumor activity against the xenograft tumor of Hela cells and had no apparent toxicity. This study highlights the advantage of introducing the medium-length amino-terminal groups at the 3-OH position of FA to enhance its anti-tumor activity and suggests that compound 4 provides a starting point for designing more potent derivatives in the future. (C) 2018 Elsevier Masson SAS. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据