Optimization of α-acylaminoketone ecdysone agonists for control of gene expression

CM Tice, RE Hormann, CS Thompson, JL Friz…

Index: Tice, Colin M.; Hormann, Robert E.; Thompson, Christine S.; Friz, Jennifer L.; Cavanaugh, Caitlin K.; Saggers, Jessica A. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 11 p. 1883 - 1886

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Citation Number: 32

Abstract

Fifteen new α-acylaminoketones were prepared by four different routes in an initial effort to optimize the potency of these compounds as ecdysone agonists. The compounds were assayed in mammalian cells expressing the ecdysone receptors from Bombyx mori (BmEcR) and Choristoneura fumiferana (CfEcR) for their ability to cause expression of a reporter gene downstream of an ecdysone response element. A new α-acylaminoketone was identified ...