Synthesis and SAR of α-Acylaminoketone ligands for control of gene expression

A lead discovery library and a follow-up focused library of α-acylaminoketones were designed based on known dibenzoylhydrazine ecdysone agonists, including GS ™–E. The compounds were assayed in mammalian cells expressing the ecdysone receptor from Bombyx mori for their ability to cause expression of...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-02, Vol.13 (3), p.475-478
Main Authors: Tice, Colin M, Hormann, Robert E, Thompson, Christine S, Friz, Jennifer L, Cavanaugh, Caitlin K, Michelotti, Enrique L, Garcia, Javier, Nicolas, Ernesto, Albericio, Fernando
Format: Article
Language:English
Subjects:
Amines - chemical synthesis
Amines - pharmacology
Animals
beta-Galactosidase - biosynthesis
beta-Galactosidase - genetics
Biological and medical sciences
Bombyx - metabolism
Cells, Cultured
Chemical control
Control
Ecdysone - pharmacology
Fundamental and applied biological sciences. Psychology
Gene Expression - drug effects
Indicators and Reagents
Ketones - chemical synthesis
Ketones - pharmacology
Lethal Dose 50
Mice
Molecular Conformation
Phytopathology. Animal pests. Plant and forest protection
Protozoa. Invertebrates
Receptors, Steroid - antagonists & inhibitors
Structure-Activity Relationship
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Summary:A lead discovery library and a follow-up focused library of α-acylaminoketones were designed based on known dibenzoylhydrazine ecdysone agonists, including GS ™–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 α-acylaminoketones were comparable to GS ™–E in this assay. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00980-0