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ID: ALA1136556

Journal: Bioorg Med Chem Lett

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

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

Abstract: 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.

CiteXplore: 12565954

DOI: 10.1016/s0960-894x(02)00980-0