| 19356928 |
Sarachine MJ, Janjic JM, Wipf P, Day BW: Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta. Bioorg Med Chem Lett. 2009 May 1;19(9):2404-8. Epub 2009 Mar 25.
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) alpha. Further screening of this library identified an ERbeta 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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