Synthesis and SAR of α-Acylaminoketone Ligands for Control of Gene Expression

Autor:	Christine S. Thompson, Javier Garcia, Fernando Albericio, Enrique Luis Michelotti, Ernesto Nicolás, Robert Eugene Hormann, Caitlin K. Cavanaugh, Colin M. Tice, Jennifer L. Friz
Rok vydání:	2003
Předmět:	Agonist Ecdysone Receptors Steroid medicine.drug_class Clinical Biochemistry Response element Molecular Conformation Pharmaceutical Science Gene Expression Biochemistry Chemical synthesis Lethal Dose 50 Mice Structure-Activity Relationship chemistry.chemical_compound Bombyx mori Drug Discovery Gene expression medicine Animals Amines Molecular Biology Cells Cultured Reporter gene biology Chemistry Organic Chemistry fungi General Medicine Ketones Bombyx beta-Galactosidase biology.organism_classification Molecular biology Molecular Medicine Indicators and Reagents Ecdysone receptor
Zdroj:	ChemInform. 34
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200320102
Popis:	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.
Databáze:	OpenAIRE
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