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

2003; Elsevier BV; Volume: 13; Issue: 3 Linguagem: Inglês

10.1016/s0960-894x(02)00980-0

1464-3405

Colin M. Tice, Robert E. Hormann, Christine S. Thompson, Jennifer L. Friz, Caitlin K. Cavanaugh, Enrique L. Michelotti, Javier Garcia, Ernesto Nicolás, Fernando Alberício,

Insect Pheromone Research and Control

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.