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Design, Synthesis and Anticancer Evaluation of New 7-O-Alkylation Genistein Derivatives
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-12-01 , DOI: 10.1007/s11094-020-02298-5
Yuyan Ren , Hongfei Chen , Xu Yao , Zehua Yang , Tingjuan Wu , Yu Guo , Junhui Xiao , Xing Zheng

Genistein is a phytoestrogen compound which possesses multiple biological activities such as anti-cancer, while its application is limited by poor pharmacokinetic properties. Structural modification is an effective approach to get genistein derivatives with better activities and approved pharmacokinetic properties. Based on previous research work, we synthesized two series of genistein derivatives bearing halogen substituents, and evaluated their inhibitory effects on the cancer cell lines MCF-7, MDA-MB-231, and MDA-MB-435. Among these derivatives, compound XI displayed the best inhibitory activity against MCF-7, MDA-MB-231 and MDA-MB-435 cell lines in vitro, which is worth further studies.

中文翻译:

新型 7-O-烷基化染料木黄酮衍生物的设计、合成和抗癌评价

染料木黄酮是一种植物雌激素化合物,具有抗癌等多种生物活性,但其药代动力学特性较差,限制了其应用。结构修饰是获得具有更好活性和经批准的药代动力学特性的染料木黄酮衍生物的有效方法。在前人研究工作的基础上,我们合成了两个系列带有卤素取代基的染料木黄酮衍生物,并评估了它们对癌细胞系MCF-7、MDA-MB-231和MDA-MB-435的抑制作用。在这些衍生物中,化合物XI在体外对MCF-7、MDA-MB-231和MDA-MB-435细胞系表现出最好的抑制活性,值得进一步研究。
更新日期:2020-12-01
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