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.
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DOI:
10.1016/s0960-894x(00)00312-7
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发表时间:
2000-08
影响因子:
2.7
通讯作者:
M. Palanki;P. Erdman;A. Manning;A. Ow;L. Ransone;C. Spooner;C. Suto;M. Suto
中科院分区:
文献类型:
--
作者:
M. Palanki;P. Erdman;A. Manning;A. Ow;L. Ransone;C. Spooner;C. Suto;M. Suto
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.