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• W2003821463 abstract "As part of our program to explore the influence of small structural modifications on the biological response of the estrogen receptor-α (ERα), we prepared and evaluated a series of mono-and di-substituted phenyl vinyl estradiols. The target compounds were prepared in 45–80% yields using the Stille coupling reaction and evaluated using competitive binding analysis with the ERα-ligand binding domain (hERα-LBD) and estrogenic activity (induction of alkaline phosphatase in Ishikawa cells). Results indicated that the 2,4- and 2,5-dimethyl derivatives, 5b and 5c, had the highest relative binding affinity (RBA = 20.5 and 37.3%) and relative stimulatory activity (RSA = 101.0% and 12.3%) of the di-methyl series." @default.
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• W2003821463 date "2012-04-01" @default.
• W2003821463 modified "2023-10-17" @default.
• W2003821463 title "Synthesis and evaluation of 17α-(dimethylphenyl)vinyl estradiols as probes of the estrogen receptor-α ligand binding domain" @default.
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• W2003821463 doi "https://doi.org/10.1016/j.steroids.2012.01.003" @default.
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