Novel inhibitors of AP-1 and NF-κB mediated gene expression: structure–activity relationship studies of ethyl 4-[(3-Methyl-2, 5-dioxo (3-pyrrolinyl)) amino]-2-( …

…, A Ow, LJ Ransone, C Spooner, C Suto, M Suto

文献索引：Palanki, Moorthy S.S.; Erdman, Paul E.; Manning, Anthony M.; Ow, Arnold; Ransone, Lynn J.; Spooner, Cheryl; Suto, Carla; Suto, Mark Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1645 - 1648

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被引用次数: 29

摘要

In an effort to identify novel inhibitors of AP-1 and NF-κB mediated transcriptional activation, several analogues of ethyl 4-[(3-methyl-2, 5-dioxo (3-pyrrolinyl)) amino]-2-(trifluoromethyl) pyrimidine-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.