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Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs)
Owen B Wallace1, Kenneth S Lauwers, Scott A Jones
1Discovery Chemistry Research and Technologies, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. wallace_owen@lilly.com
Bioorganic & Medicinal Chemistry Letters
|May 17, 2003
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.