Abstract
Screening of our in-house compound library comprised of intermediates of natural product synthesis projects resulted in discovering two novel gamma-secretase inhibitors, which coincidently had similar moieties, that is, cyclohexenone and two aryl groups arranged on the core six-membered ring. Structure-activity relationship studies of these compounds were also developed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amyloid Precursor Protein Secretases
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Biological Products / chemistry*
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Biological Products / pharmacology
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Cyclohexanones / chemistry
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Cyclohexanones / pharmacology
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Dioxoles / chemistry
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Endopeptidases / metabolism*
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Heterocyclic Compounds / chemistry
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Inhibitory Concentration 50
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
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Tacrolimus / chemistry
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Tacrolimus / pharmacology
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Tetrahydroisoquinolines / chemistry
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Trabectedin
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Vinblastine / chemistry
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Vinblastine / pharmacology
Substances
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Biological Products
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Cyclohexanones
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Dioxoles
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Heterocyclic Compounds
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Protease Inhibitors
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Tetrahydroisoquinolines
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Vinblastine
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Amyloid Precursor Protein Secretases
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Endopeptidases
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Trabectedin
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Tacrolimus