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Discovery of BGJ398 (3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

Guagnano, Vito and Furet, Pascal and Spanka, Carsten and Bordas, Vincent and Le Douget, Mickael and Stamm, Christelle and Molle, Sandra and Brueggen, Josef and Schmid, Herbert and Jensen, Michael Rugaard and Schnell, Christian and Wartmann, Markus and Berghausen, Joerg and Drueckes, Peter and Zimmerlin, Alfred Gilbert and Bussiere, Dirksen and Murray, Jeremy and Graus Porta, Diana (2011) Discovery of BGJ398 (3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase. Journal of Medicinal Chemistry, 54 (20). pp. 7066-7083. ISSN 0022-2623

Abstract

A novel series of aryl pyrimidin-4-yl ureas has been optimized to afford potent and selective inhibitors of the fibroblast growth factor receptor tyrosine kinases 1, 2 and 3, by rationally designing the substitution pattern of the aryl ring. On the basis of its in vitro profile, compound 2h was selected for in vivo evaluation and showed significant antitumor activity in RT112 bladder cancer xenografts models overexpressing wild-type FGFR3. These results support the potential therapeutic use of 2h as a new anticancer agent.

Item Type: Article
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Date Deposited: 13 Oct 2015 13:15
Last Modified: 13 Oct 2015 13:15
URI: https://oak.novartis.com/id/eprint/4874

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