4.7 Article

Synthesis and biological evaluation of novel withangulatin A derivatives as potential anticancer agents

期刊

BIOORGANIC CHEMISTRY
卷 108, 期 -, 页码 -

出版社

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2021.104690

关键词

Withangulatin A derivatives; Anticancer; Cell cycle; Apoptosis; Reactive oxygen species

资金

  1. National Natural Science Foundation of China [81872983]
  2. Natural Science Foundation of Jiangsu Province [BK20181329]
  3. Drug Innovation Major Project [2018ZX09711-001-007]

向作者/读者索取更多资源

Novel derivatives of withangulatin A (WA) were synthesized and evaluated for their antiproliferative activity against four human cancer cell lines, with compound 10 showing the most potent activity against the human breast cancer cell line MDA-MB-231. Compound 10 also demonstrated a high selectivity index for breast cancer MDA-MB-231 cells, indicating its potential as a promising anticancer agent.
Novel withangulatin A (WA) derivatives were synthesized and evaluated for antiproliferative activity against four human cancer cell lines (U2OS, MDA-MB-231, HepG2, and A549). Among these derivatives, 10 exhibited the most potent antiproliferative activity, with an IC50 value of 74.0 nM against the human breast cancer cell line MDA-MB-231 and potency that was 70-fold that of WA (IC50 = 5.22 mu M). Moreover, 10 caused G2-phase cell cycle arrest in a concentration-dependent manner and induced the apoptosis of MDA-MB-231 cells by increasing intracellular reactive oxygen species (ROS). Compound 10 showed a high selectivity index (SI = 267.03) for breast cancer MDA-MB-231 cells. These results suggest that 10 is a promising anticancer agent.

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。

评论

主要评分

4.7
评分不足

次要评分

新颖性
-
重要性
-
科学严谨性
-
评价这篇论文

推荐

暂无数据
暂无数据