Title |
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
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Published in |
Journal of Medicinal Chemistry, September 2011
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DOI | 10.1021/jm2006222 |
Pubmed ID | |
Authors |
Vito Guagnano, Pascal Furet, Carsten Spanka, Vincent Bordas, Mickaël Le Douget, Christelle Stamm, Josef Brueggen, Michael R. Jensen, Christian Schnell, Herbert Schmid, Markus Wartmann, Joerg Berghausen, Peter Drueckes, Alfred Zimmerlin, Dirksen Bussiere, Jeremy Murray, Diana Graus Porta |
Abstract |
A novel series of N-aryl-N'-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 1h (NVP-BGJ398) 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 1h as a new anticancer agent. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 1 | 100% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 1 | 100% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 2 | 1% |
Unknown | 168 | 99% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 35 | 21% |
Researcher | 31 | 18% |
Student > Bachelor | 15 | 9% |
Student > Postgraduate | 12 | 7% |
Student > Master | 12 | 7% |
Other | 30 | 18% |
Unknown | 35 | 21% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 34 | 20% |
Biochemistry, Genetics and Molecular Biology | 31 | 18% |
Medicine and Dentistry | 24 | 14% |
Agricultural and Biological Sciences | 20 | 12% |
Pharmacology, Toxicology and Pharmaceutical Science | 14 | 8% |
Other | 13 | 8% |
Unknown | 34 | 20% |