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Estrogen receptor dependent inhibitors of NF-κB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives : pathway selective inhibitors of NF-κB, a potential treatment for rheumatoid arthritis

Caggiano, Thomas J. and Brazzale, Antony and Ho, Douglas M. and Kraml, Christina M. and Trybulski, Eugene and Chadwick, Christopher C. and Chippari, Sue and Borges-Marcucci, Lisa and Eckert, Amy and Keith, James C. and Kenney, Thomas and Harnish, Douglas C.. (2007) Estrogen receptor dependent inhibitors of NF-κB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives : pathway selective inhibitors of NF-κB, a potential treatment for rheumatoid arthritis. Journal of medicinal chemistry, Vol. 50, no. 22. pp. 5245-5248.

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Official URL: http://edoc.unibas.ch/dok/A5253448

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Abstract

Pathway selective ligands of the estrogen receptor inhibit transcriptional activation of proinflammatory genes mediated by NF-kappaB. Substituted 2-cyanopropanoic acid derivatives were developed leading to the discovery of WAY-204688, an orally active, pathway selective, estrogen receptor dependent anti-inflammatory agent. This propanamide was shown to be orally active in preclinical models of inflammatory diseases, such as rheumatoid arthritis, without the proliferative effect associated with traditional estrogens.
Faculties and Departments:03 Faculty of Medicine > Bereich Psychiatrie (Klinik) > Erwachsenenpsychiatrie UPK
03 Faculty of Medicine > Departement Klinische Forschung > Bereich Psychiatrie (Klinik) > Erwachsenenpsychiatrie UPK
UniBasel Contributors:Eckert, Anne
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:American Chemical Society
ISSN:0022-2623
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:22 Mar 2012 14:23
Deposited On:22 Mar 2012 13:36

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