Tetrahydroquinoline-based selective estrogen receptor modulators (SERMs) |
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| Authors: | Wallace Owen B Lauwers Kenneth S Jones Scott A Dodge Jeffrey A |
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| Affiliation: | Discovery Chemistry Research and Technologies, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. wallace_owen@lilly.com |
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| 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. |
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