Author(s): Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, , Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M,
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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.
This article was published in J Med Chem
and referenced in Journal of Cancer Science & Therapy