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 …
V Guagnano, P Furet, C Spanka, V Bordas… - Journal of medicinal …, 2011 - ACS Publications
V Guagnano, P Furet, C Spanka, V Bordas, M Le Douget, C Stamm, J Brueggen, MR Jensen…
Journal of medicinal chemistry, 2011•ACS PublicationsA 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.
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.
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.
ACS Publications