Synthesis and activity of a new class of pathway-selective estrogen receptor ligands: hydroxybenzoyl-3,4-dihydroquinoxalin-2(1H)-ones |
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| Authors: | Mahaney Paige E Webb Michael B Ye Fei Sabatucci Joseph P Steffan Robert J Chadwick Christopher C Harnish Douglas C Trybulski Eugene J |
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| Affiliation: | Chemical and Screening Sciences, Wyeth Research, Discovery Medicinal Chemistry, 500 Arcola Road, Collegeville, PA 19465, USA. mahanep@wyeth.com |
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| Abstract: | The anti-inflammatory activity of non-selective estrogens has been attributed to their ability to antagonize the activity of nuclear factor kappaB (NF-kappaB), a known mediator of inflammatory responses. Here we report the identification of a potent new class of pathway-selective ER ligands that selectively antagonize NF-kappaB functional activity, while exhibiting a lack of classical estrogenic effect. |
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