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-kappaB mediated gene expression.

Autor: Palanki MS; Celgene Signal Research Division, 5555 Oberlin Drive, San Diego, CA 92121, USA. mpalanki@signalpharm.com, Gayo-Fung LM, Shevlin GI, Erdman P, Sato M, Goldman M, Ransone LJ, Spooner C
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Sep 16; Vol. 12 (18), pp. 2573-7.
DOI: 10.1016/s0960-894x(02)00517-6
Abstrakt: 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-kappaB 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.
Databáze: MEDLINE
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