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1: Bioorg Med Chem Lett. 2003 Feb 10;13(3):475-8.Click here to read Links

Synthesis and SAR of alpha-acylaminoketone ligands for control of gene expression.

Tice CM, Hormann RE, Thompson CS, Friz JL, Cavanaugh CK, Michelotti EL, Garcia J, Nicolas E, Albericio F.

RHeoGene, PO Box 949, 727Norristown Road, Spring House, PA 19477-0949, USA. ctice@rheogene.com

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.

PMID: 12565954 [PubMed - indexed for MEDLINE]