Synthesis of Sea Cucumber Saponins with Antitumor Activities.,The Journal of Organic Chemistry

当前位置： X-MOL 学术 › J. Org. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis of Sea Cucumber Saponins with Antitumor Activities.
The Journal of Organic Chemistry ( IF 3.3 ) Pub Date : 2020-09-14 , DOI: 10.1021/acs.joc.0c01191
Xiaofei Shao ₁ , Xiaobo Wang ₂ , Kaidi Zhu ₁ , Yongjun Dang ₂ , Biao Yu _{1,

3}

Affiliation

Holostane glycosides are characteristic metabolites of sea cucumbers, which possess various biological activities. Here, we report the synthesis of two representative congeners, namely, pervicoside B and C, starting from lanosterol with the longest linear sequence of both 34 steps and in 0.3% overall yields. The flexible synthetic approach has enabled us to expeditiously prepare 16 analogues for preliminary studies on the key structural features influencing their antiproliferative activities against tumor cells. A simplified disaccharide is found to be as potent as natural tetrasaccharides, which can be used as a lead for future studies.

中文翻译：

具有抗肿瘤活性的海参皂苷的合成。

甾烷糖苷是海参的特征代谢产物，具有多种生物活性。在这里，我们报告了两种代表性同类物的合成，即pervicoside B和C，它是从羊毛甾醇开始的，其线性最长的序列均为34个步骤，总产率为0.3％。灵活的合成方法使我们能够迅速制备出16种类似物，以初步研究影响其抗肿瘤细胞增殖活性的关键结构特征。发现简化的二糖与天然四糖一样有效，可用作未来研究的先导。

更新日期：2020-10-02

点击分享查看原文

点击收藏

阅读更多本刊最新论文