European Journal of Medicinal Chemistry p. 328 - 339 (2016)
Update date:2022-08-02
Topics:
Tang, Zhichao
Wu, Chengzhe
Wang, Tianlin
Lao, Kejing
Wang, Yejun
Liu, Linyi
Muyaba, Moses
Xu, Pei
He, Conghui
Luo, Guoshun
Qian, Zhouyang
Niu, Shaoxiong
Wang, Lijun
Wang, Ying
Xiao, Hong
You, Qidong
Xiang, Hua
The estrogen receptors have played important roles in breast cancer development and progression. Selective estrogen receptor modulators, such as Tamoxifen, have showed great benefits in the treatment and prevention of breast cancer. But the disadvantages of induction of endometrial cancer and drug resistance have limited their use. Multiple ligand which act at multiple biomolecular targets may exert favorable advantages of improved efficacy with lower incidence of side effects. In this work, we described the synthesis and evaluation of a series of 6-aryl-indenoisoquinolone derivatives as dual ERα and VEGFR-2 inhibitors. These compounds presented good ERα binding affinity and ERα antagonistic activity, as well as potent VEGFR-2 inhibitory potency. They also possessed excellent anti-proliferative activities against MCF-7, MDA-MB-231, Ishikawa and HUVEC cell lines. Further investigation of selective compound 21c showed that it was able to inhibit the activation of VEGFR-2 and the signaling transduction of Raf-1/MAPK/ERK pathway in MCF-7 cells.
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