Optimization of α-acylaminoketone ecdysone agonists for control of gene expression
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) fo...
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Published in | Bioorganic & medicinal chemistry letters Vol. 13; no. 11; pp. 1883 - 1886 |
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Main Authors | , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
02.06.2003
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 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.
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Bibliography: | ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(03)00315-9 |