The DOI matches its Crossref record; 48 of the 48 references it cites were found in a registry or an index.
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
Open accessAbstract
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.
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Cites
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Cited by
Arai, Y., Totoki, Y., Hosoda, F., Shirota, T., Hama, N., Nakamura, H., Ojima, H., Furuta, K., Shimada, K., Okusaka, T., et al. (2014) · Hepatology · doi:10.1002/hep.26890 · Cited by 553
Fibroblasts in cancer: Unity in heterogeneity
Chhabra, Y., & Weeraratna, A. T. (2023) · Cell · doi:10.1016/j.cell.2023.03.016 · Cited by 474
Nogova, L., Sequist, L. V., Perez Garcia, J. M., Andre, F., Delord, J.-P., Hidalgo, M., Schellens, J. H. M., Cassier, P. A., Camidge, D. R., Schuler, M., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2016.67.2048 · Cited by 432
Self-citationJavle, M., Roychowdhury, S., Kelley, R. K., Sadeghi, S., Macarulla, T., Weiss, K. H., Waldschmidt, D.-T., Goyal, L., Borbath, I., El-Khoueiry, A., et al. (2021) · The Lancet Gastroenterology & Hepatology · doi:10.1016/s2468-1253(21)00196-5 · Cited by 428
Dieci, M. V., Arnedos, M., Andre, F., & Soria, J. C. (2013) · Cancer Discovery · doi:10.1158/2159-8290.cd-12-0362 · Cited by 406
Metadata
- Authors
- Guagnano, V., Furet, P., Spanka, C., Bordas, V., Le Douget, M., Stamm, C., Brueggen, J., Jensen, M. R., Schnell, C., Schmid, H., Wartmann, M., Berghausen, J., Drueckes, P., Zimmerlin, A., Bussiere, D., Murray, J., & Graus Porta, D.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2011-09-21
- Volume
- 54
- Issue
- 20
- Pages
- 7066-7083
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2093090488
- Cited by
- 477
- References
- 48
- FWCI
- 7.99
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: 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. https://app.cochat.ai/papers/10.1021/jm2006222
- The paper
- Guagnano, V., Furet, P., Spanka, C., Bordas, V., Le Douget, M., Stamm, C., Brueggen, J., Jensen, M. R., Schnell, C., Schmid, H., Wartmann, M., Berghausen, J., Drueckes, P., Zimmerlin, A., Bussiere, D., Murray, J., & Graus Porta, D. (2011). 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. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm2006222
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
