Synthesis of 2-Phenylbenzofuran Derivatives and Selective Binding Activities on Estrogen Receptor

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概要

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• An improved chemical reaction protocol with short time and easy work-up was described here for 2-phenylbenzofuran derivatives. The final purified products, 2-phenylbenzofuran derivatives 5a—g and the intermediate diols 4a—g, were evaluated for their estrogen receptor (ER) binding affinity and selective activity in vitro. Among these fourteen tested compounds, 4g and 5g showed higher binding affinity on ER subtypes, ERα and ERβ. Compound 4g exhibited preferable ERα binding, while 5g was more estrogen selective for ERβ. The molecular docking was also performed to explore the detailed interactive interface between ER and the compounds.

著者

• Shen Zhengrong

  Institute of Materia Medica, Zhejiang Academy of Medical Sciences

• Ma Zhen

  Institute of Materia Medica, Zhejiang Academy of Medical Sciences

• Huang Wenhai

  Institute of Materia Medica, Zhejiang Academy of Medical Sciences

• Zhang Ping

  Institute of Materia Medica, Zhejiang Academy of Medical Sciences

• Yang Yewei

  Institute of Materia Medica, Zhejiang Academy of Medical Sciences

• Zheng Xiaoliang

  Center for Translational Molecular Medicine, Zhejiang Academy of Medical Sciences

関連論文

• Synthesis of 2-Phenylbenzofuran Derivatives and Selective Binding Activities on Estrogen Receptor

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