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

…, EL Michelotti, J Garcia, E Nicolas, F Albericio

Index: Tice, Colin M.; Hormann, Robert E.; Thompson, Christine S.; Friz, Jennifer L.; Cavanaugh, Caitlin K.; Michelotti, Enrique L.; Garcia, Javier; Nicolas, Ernesto; Albericio, Fernando Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 3 p. 475 - 478

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Citation Number: 30

Abstract

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 ...