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
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Guagnano, Vito, Furet, Pascal, Spanka, Carsten, Bordas, Vincent, Le Douget, Mickael, Stamm, Christelle, Molle, Sandra, Brueggen, Josef, Schmid, Herbert, Jensen, Michael Rugaard, Schnell, Christian, Wartmann, Markus, Berghausen, Joerg, Drueckes, Peter, Zimmerlin, Alfred Gilbert, Bussiere, Dirksen, 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 |