Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).

Article Details

Citation

Copy to clipboard

Wallace OB, Lauwers KS, Jones SA, Dodge JA

Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs).

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1907-10.

PubMed ID

12749895 [ View in PubMed

]

Abstract

A new series of estrogen receptor ligands based on a 6-hydroxy-tetrahydroquinoline scaffold is described, in addition to their binding affinity and functional activity in MCF-7 cells. Several 1,2-disubstituted tetrahydroquinolines bearing a basic side chain were shown to be high affinity ligands and antagonists in the MCF-7 proliferation assay. Compounds lacking the basic side chain were agonists in the MCF-7 assay.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Raloxifene	Estrogen receptor alpha	Ki (nM)	0.4	N/A	N/A	Details
Raloxifene	Estrogen receptor beta	Ki (nM)	4.3	N/A	N/A	Details