Synthesis and anti-tumor activity of menthylamine derivatives: Focusing on the potent inhibitory effect of compound W8 on glioma growth

IF 3.3 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Xiaoran Wu , Yanhang Zhuo , Jiangjian Liu , Ziming He , Meiling Wang , Wenjun Lei , Qiong Liang , Aidong Wang , Zhiyi Shen , Sunhui Chen , Shihao Zheng , Huihui Huang
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引用次数: 0

Abstract

In this work, we successfully synthesized eight distinct compounds, comprising four chiral menthylamines and related derivatives. We evaluated their cytotoxic potential against a panel of human cancer cell lines, including human colon cancer HCT-116 cells, human esophageal squamous KYSE-150 cells, human breast cancer MCF-7 cells, and human glioma U87 cells. The U87 cells were chosen for a more in-depth investigation of their anti-tumor efficacy. Further exploration of the cytotoxicity mechanisms was conducted, complemented by in vivo studies using mice bearing tumors. These analyses unveiled the possible mechanisms by which menthylamide derivatives exert their anti-tumor effects. Notably, compound W8 demonstrated a potent inhibitory action against the proliferation of brain glioma cells. The findings from this research provide valuable insights that pave the way for the future application of menthylamides in cancer therapeutics.

Abstract Image

甲胺衍生物的合成及抗肿瘤活性:重点研究化合物W8对胶质瘤生长的抑制作用
在这项工作中,我们成功地合成了八种不同的化合物,包括四种手性甲胺及其衍生物。我们评估了它们对一组人类癌细胞系的细胞毒性潜力,包括人类结肠癌HCT-116细胞、人类食管鳞状细胞KYSE-150细胞、人类乳腺癌MCF-7细胞和人类胶质瘤U87细胞。选择U87细胞进行更深入的抗肿瘤效果研究。进一步探索细胞毒性机制,并辅以小鼠体内肿瘤研究。这些分析揭示了甲基酰胺衍生物发挥其抗肿瘤作用的可能机制。值得注意的是,化合物W8显示出对脑胶质瘤细胞增殖的有效抑制作用。这项研究的发现提供了有价值的见解,为未来甲基胺在癌症治疗中的应用铺平了道路。
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来源期刊
Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry 医学-生化与分子生物学
CiteScore
6.80
自引率
2.90%
发文量
413
审稿时长
17 days
期刊介绍: Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.
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