1. Academic Validation
  2. Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression

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

  • Bioorg Med Chem Lett. 2003 Jun 2;13(11):1883-6. doi: 10.1016/s0960-894x(03)00315-9.
Colin M Tice 1 Robert E Hormann Christine S Thompson Jennifer L Friz Caitlin K Cavanaugh Jessica A Saggers
Affiliations

Affiliation

  • 1 RHeoGene, PO Box 949, 727 Norristown Road, Spring House, PA 19477-0949, USA. ctice@concurrentpharma.com
Abstract

Fifteen new alpha-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 alpha-acylaminoketone was identified which had activity equal to that of the standard dibenzoylhydrazine ecdysone agonist GS()-E in the assay based on CfEcR.

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