染料木素邻苯二甲酰亚胺衍生物合成及其抗乳腺癌活性研究
Synthesis and anti-breast cancer activity of phthalimide derivatives of genistein
郑兴 1孙林军 1朱颖丽 2姚旭3
作者信息
- 1. 湖南科技职业学院,湖南 长沙 410004
- 2. 南华大学药学院,湖南 衡阳 421001;中南大学湘雅药学院,湖南 长沙 410013
- 3. 南华大学药学院,湖南 衡阳 421001
- 折叠
摘要
目的 研究染料木素邻苯二甲酰亚胺衍生物的体外抗乳腺癌活性及其作用机制.方法 合成染料木素邻苯二甲酰亚胺衍生物,通过MTT法检测其对癌细胞株MCF-7、MBA-MD-231、MBA-MD-435 增殖抑制作用;并通过分子对接的方法探讨染料木素邻苯二甲酰亚胺衍生物与雌激素受体α(ERα)的作用方式.结果 合成了3 个染料木素邻苯二甲酰亚胺衍生物,并对其生物活性及抗乳腺癌机制进行了验证.结论 染料木素邻苯二甲酰亚胺衍生物具有较强的抗乳腺癌活性,可能与竞争性抑制ERα等机制有关.
Abstract
Objective To study the anti-breast cancer activity and mechanism of phthalimide derivatives of genistein in vitro.Methods Phthalimide derivatives of genistein were prepared and their anti-proliferative effects of MCF-7,MDA-MB-231,MDA-MB-435,and MCF-10A cell lines were evaluated by standard MTT method.Molecular docking was used to explore the interaction between the synthesized compounds and estrogen receptor α(ERα).Results Three phthalimide derivatives of genistein were synthesized and their bioactivity and anti-breast cancer mechanism were verified.Conclusion The designed phthalimide derivatives of genistein possess potent anti-breast cancer activity may act as competitive inhibition of ERα and other mechanisms.
关键词
染料木素/邻苯二甲酰亚胺/衍生物/抗乳腺癌活性/分子对接Key words
Genistein/Phthalimide/Derivatives/Anti-breast cancer activities/Molecular docking引用本文复制引用
基金项目
湖南省自然科学基金(2020JJ6052)
湖南省自然科学基金(2021JJ80015)
中国科学院有机氟化学重点实验室项目(2018-10)
出版年
2024
国家科技期刊平台
NSTL
万方数据