European Journal of Medicinal Chemistry p. 135 - 148 (2019)
Update date:2022-08-17
Topics:
Wang, Cong
Li, Leilei
Fu, Dongyang
Qin, Tiantian
Ran, Yange
Xu, Feng
Du, Xinrui
Gao, Haiying
Sun, Shuaijun
Yang, Tengjiao
Zhang, Xueyan
Huo, Junfeng
Zhao, Wen
Zhang, Zhenzhong
Shi, Xiufang
Angiogenesis plays an essential role in tumourigenesis and tumour progression, and anti-angiogenesis therapies have shown promising antitumour effects in solid tumours. 2-Methoxyestradiol (2ME2), an endogenous metabolite of estradiol, has been regarded as a potential antitumour agent mainly targeting angiogenesis. Here we synthesized a novel series of chalcones based on 2-methoxyestradiol and evaluated their potential activities against tumours. Compound 11e was demonstrated to have potent antiangiogenic activity. Further studies showed that 11e suppressed tumour growth in human breast cancer (MCF-7)xenograft models without obvious side effects. Evaluation of the mechanism revealed that 11e targeted the epithelial to mesenchymal transition (EMT)process in MCF-7 cells and inhibited HUVEC migration and then contributed to hindrance of angiogenesis. Thus, 11e may be a promising antitumour agent with excellent efficacy and low toxicity.
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