Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.

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Blizzard TA, DiNinno F, Chen HY, Kim S, Wu JY, Chan W, Birzin ET, Yang YT, Pai LY, Hayes EC, DaSilva CA, Rohrer SP, Schaeffer JM, Hammond ML

Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3912-6.

PubMed ID

15993065 [ View in PubMed

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Abstract

An optimized side chain for dihydrobenzoxathiin SERAMs was discovered and attached to four dihydrobenzoxathiin platforms. The novel SERAMs show exceptional estrogen antagonist activity in uterine tissue and an MCF-7 breast cancer cell assay.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor beta	IC 50 (nM)	1.1	N/A	N/A	Details
Raloxifene	Estrogen receptor beta	IC 50 (nM)	1.9	N/A	N/A	Details