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

Zhang P,Yang Y,Zheng X,Huang W,Ma Z,Shen Z

doi

10.1248/cpb.60.270

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

270-4

issue

2

eissn

0009-2363

issn

1347-5223

pii

JST.JSTAGE/cpb/60.270

journal_volume

60

pub_type

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