Abstract
In an effort to identify novel inhibitors of AP-1 and NF-kappaB mediated transcriptional activation, several analogues of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)pyr imidine-5-carboxylate (1) were synthesized and tested in two in vitro assays. The 2-(2'-thienyl) substituted compound (11) was identified as the most potent in this series.
MeSH terms
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Gene Expression Regulation / drug effects*
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Humans
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Jurkat Cells
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Maleimides / chemistry
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Maleimides / pharmacology*
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NF-kappa B / antagonists & inhibitors*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
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Transcription Factor AP-1 / antagonists & inhibitors*
Substances
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Maleimides
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NF-kappa B
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Pyrimidines
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Transcription Factor AP-1
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ethyl 4-(3-methyl-2,5-dioxo(3-pyrrolinyl)amino)-2-(trifluoromethyl)pyrimidine-5-carboxylate