Novel inhibitors of AP-1 and NF-kappaB mediated gene expression: structure-activity relationship studies of ethyl 4-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-2-(trifluoromethyl)++ +pyrimidi ne-5-carboxylate

  • Bioorg Med Chem Lett. 2000 Aug 7;10(15):1645-8. doi: 10.1016/s0960-894x(00)00312-7.
M S Palanki  1 ,  P E Erdman ,  A M Manning ,  A Ow ,  L J Ransone ,  C Spooner ,  C Suto ,  M Suto
Affiliations
PMID: 10937715 DOI: 10.1016/s0960-894x(00)00312-7
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.

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