Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.

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Chen HY, Kim S, Wu JY, Birzin ET, Chan W, Yang YT, Dahllund J, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML

Estrogen receptor ligands. Part 3: The SAR of dihydrobenzoxathiin SERMs.

Bioorg Med Chem Lett. 2004 May 17;14(10):2551-4.

PubMed ID

15109649 [ View in PubMed

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Abstract

A series of 3-alkyl, 3-cycloalkyl, and 3-heteroaryl dihydrobenzoxathiin analogs 1 were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. In general, the compounds were found to exhibit a high degree of selectivity for ER alpha over ER beta, but were less potent than the original lead compound 1a in the inhibition of estradiol-driven uterine proliferation.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Compound 4-D	Estrogen receptor alpha	IC 50 (nM)	3.1	N/A	N/A	Details
Raloxifene	Estrogen receptor alpha	IC 50 (nM)	1.8	N/A	N/A	Details
Raloxifene	Estrogen receptor beta	IC 50 (nM)	12	N/A	N/A	Details