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

作　　者：郑兴 孙林军 朱颖丽 姚旭 ZHENG Xing;SUN Linjun;ZHU Yingli;YAO Xu(Hunan Vocational College of Science and Technology,Changsha 410004,China;School of Pharmaceutical Sciences,University of South China,Hengyang 421001,China;Xiangya School of Pharmaceutical Sciences,Central South University,Changsha 410013,China)

机构地区：[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 [3]中南大学湘雅药学院,湖南长沙410013

出　　处：《药学研究》2024年第5期435-438,454,共5页Journal of Pharmaceutical Research

基　　金：湖南省自然科学基金项目(No.2020JJ6052、2021JJ80015);中国科学院有机氟化学重点实验室(No.2018-10);。

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。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 receptorα(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 ERαand 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 

分 类 号：R914.5[医药卫生—药物化学]