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 …

…, LM Gayo-Fung, GI Shevlin, P Erdman, M Sato…

文献索引：Palanki, Moorthy S.S.; Gayo-Fung, Leah M.; Shevlin, Graziella I.; Erdman, Paul; Sato, Mark; Goldman, Mark; Ransone, Lynn J.; Spooner, Cheryl Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 18 p. 2573 - 2577

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被引用次数: 48

摘要

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.