Abstract
A lead discovery library and a follow-up focused library of alpha-acylaminoketones were designed based on known dibenzoylhydrazine ecdysone agonists, including GS(TM)-E. The compounds were assayed in mammalian cells expressing the ecdysone receptor from Bombyx mori for their ability to cause expression of a reporter gene downstream of an ecdysone response element. The most potent alpha-acylaminoketones were comparable to GS(TM)-E in this assay.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Amines / chemical synthesis*
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Amines / pharmacology*
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Animals
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Bombyx / metabolism
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Cells, Cultured
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Ecdysone / pharmacology
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Gene Expression / drug effects*
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Indicators and Reagents
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Ketones / chemical synthesis*
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Ketones / pharmacology*
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Lethal Dose 50
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Mice
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Molecular Conformation
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Receptors, Steroid / antagonists & inhibitors
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Structure-Activity Relationship
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beta-Galactosidase / biosynthesis
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beta-Galactosidase / genetics
Substances
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Amines
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Indicators and Reagents
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Ketones
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Receptors, Steroid
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ecdysone receptor
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Ecdysone
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beta-Galactosidase