551963-98-5Relevant academic research and scientific papers
Synthesis and SAR of α-acylaminoketone ligands for control of gene expression
Tice, Colin M.,Hormann, Robert E.,Thompson, Christine S.,Friz, Jennifer L.,Cavanaugh, Caitlin K.,Michelotti, Enrique L.,Garcia, Javier,Nicolas, Ernesto,Albericio, Fernando
, p. 475 - 478 (2007/10/03)
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.
Optimization of α-acylaminoketone ecdysone agonists for control of gene expression
Tice, Colin M.,Hormann, Robert E.,Thompson, Christine S.,Friz, Jennifer L.,Cavanaugh, Caitlin K.,Saggers, Jessica A.
, p. 1883 - 1886 (2007/10/03)
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 which had activity equal to that of the standard dibenzoylhydrazine ecdysone agonist GS-E in the assay based on CfEcR.
