BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.

@article{Nourry2010BRAFIB,
  title={BRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring.},
  author={Arnaud Nourry and Alfonso Zambon and Lawrence C Davies and Ion Niculescu-Duvaz and Harmen P Dijkstra and Delphine M{\'e}nard and Catherine Gaulon and Dan Niculescu-Duvaz and Bart M.J.M. Suijkerbuijk and Frank Friedlos and Helen A. Manne and Ruth S. Kirk and Steven Whittaker and Richard Marais and Caroline J. Springer},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 5},
  pages={1964-78}
}
We recently reported on the development of a novel series of BRAF inhibitors based on a tripartite A-B-C system characterized by a para-substituted central aromatic core connected to an imidazo[4,5]pyridin-2-one scaffold and a substituted urea linker. Here, we present a new series of BRAF inhibitors in which the central phenyl ring connects to the hinge binder and substrate pocket of BRAF with a meta-substitution pattern. The optimization of this new scaffold led to the development of low… CONTINUE READING