2. Academic Validation
  3. 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

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

Affiliation

  • 1 Signal Pharmaceuticals, Inc., San Diego, CA 92121, USA. mpalanki@signalpharm.com
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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