Tetrahydroquinoline-Based selective estrogen receptor modulators (SERMs)

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-06, Vol.13 (11), p.1907-1910
Main Authors: Wallace, Owen B, Lauwers, Kenneth S, Jones, Scott A, Dodge, Jeffrey A
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cell Division - drug effects
Cell Line, Tumor
Hormones. Endocrine system
Humans
Hydroxyquinolines - chemical synthesis
Hydroxyquinolines - chemistry
Hydroxyquinolines - pharmacology
Inhibitory Concentration 50
Ligands
Medical sciences
Pharmacology. Drug treatments
Receptors, Estrogen - agonists
Receptors, Estrogen - antagonists & inhibitors
Receptors, Estrogen - metabolism
Selective Estrogen Receptor Modulators - chemical synthesis
Selective Estrogen Receptor Modulators - chemistry
Selective Estrogen Receptor Modulators - pharmacology
Structure-Activity Relationship
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Summary: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. The synthesis of a series of 6-hydroxy-tetrahydroquinoline-based estrogen receptor ligands is disclosed. Binding affinity and inhibition of MCF-7 breast adenocarcinoma cell proliferation is discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00306-8