Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.

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Dykstra KD, Guo L, Birzin ET, Chan W, Yang YT, Hayes EC, DaSilva CA, Pai LY, Mosley RT, Kraker B, Fitzgerald PM, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML

Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2322-8. Epub 2007 Jan 25.

PubMed ID

17289385 [ View in PubMed

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Abstract

A novel class of indole ligands for estrogen receptor alpha have been discovered which exhibit potent affinity and high selectivity. Substitution of the bazedoxifene skeleton to the linker present in the HTS lead 1a provided 22b which was found to be 130-fold alpha-selective and acted as an antagonist of estradiol activity in uterine tissue and MCF-7 cancer cells.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Estradiol	Estrogen receptor alpha	IC 50 (nM)	1	N/A	N/A	Details
Estradiol	Estrogen receptor beta	IC 50 (nM)	1	N/A	N/A	Details
N-[(1R)-3-(4-HYDROXYPHENYL)-1-METHYLPROPYL]-2-(2-PHENYL-1H-INDOL-3-YL)ACETAMIDE	Estrogen receptor alpha	IC 50 (nM)	1	N/A	N/A	Details