title: Synthesis of 2-phenylbenzofuran derivatives and selective binding activities on estrogen receptor.
abstract: 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.
authors.affiliation: Institute of Materia Medica, Zhejiang Academy of Medical Sciences, Hangzhou, China.
authors.forename: Ping
authors.initials: P
authors.lastname: Zhang
authors.forename: Yewei
authors.initials: Y
authors.lastname: Yang
authors.forename: Xiaoliang
authors.initials: X
authors.lastname: Zheng
authors.forename: Wenhai
authors.initials: W
authors.lastname: Huang
authors.forename: Zhen
authors.initials: Z
authors.lastname: Ma
authors.forename: Zhengrong
authors.initials: Z
authors.lastname: Shen
mesh_terms: D001572:Benzofurans / Q000138:chemical synthesis* / Q000737:chemistry; D047628:Estrogen Receptor alpha / Q000819:agonists*; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015394:Molecular Structure; D010636:Phenols / Q000138:chemical synthesis* / Q000737:chemistry; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D001572:Benzofurans; C506487:ESR1 protein, human; D047628:Estrogen Receptor alpha; D010636:Phenols