Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor β

The C-cyclopropylalkylamide scaffold was previously identified as a new structural framework for antiestrogens. A second generation library provided three compounds that bind estrogen receptor (ER)α. Further screening of this library identified an ERβ hit and inspired another round of SAR. A new focused library was tested for binding to the ERs, and for effects on the growth of breast cancer cell lines and protein levels of common cell cycle regulators.

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