Structure-activity relationship studies of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine- 5-carboxylate: An inhibitor of AP-1 and NF-κB mediated gene expression
Several analogues of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine- 5-carboxylate (1) were synthesized and tested as inhibitors of AP-1 and NF-κB mediated transcriptional activation in Jurkat T cells. From our SAR work, ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))-N-methylamino]-4-(trifluoromethyl)- pyrimidine-5-carboxylate was identified as a novel and potent inhibitor.
Synthesis and solid-state polymerization of 5-(2-methylthio4-methylpyrimidin-5-yl)penta-2,4-diyn-l-ol and of several of its derivatives
5-(2-Methylthio-4-methylpyrimidin-5-yl)penta-2,4-diyn-1-ol was synthesized by asymmetric coupling, and the corresponding diacetylene monomers were also prepared in good yields. These monomers could be dissolved in common organic solvents. The monomers can be polymerized in the solid state using heat, light or y-radiation. In addition, micro- and macroscopic third-order susceptibilities were measured by the degenerate four-wave mixing (DFWM) method for the yielded polymers. The Royal Society of Chemistry 2000.