The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase

  • Bioorg Med Chem Lett. 2008 Aug 1;18(15):4373-6. doi: 10.1016/j.bmcl.2008.06.070.
Andrew K Takle  1 ,  Mark J Bamford ,  Susannah Davies ,  Robert P Davis ,  David K Dean ,  Alessandra Gaiba ,  Elaine A Irving ,  Frank D King ,  Antoinette Naylor ,  Christopher A Parr ,  Alison M Ray ,  Alastair D Reith ,  Beverley B Smith ,  Penelope C Staton ,  Jon G A Steadman ,  Tania O Stean ,  David M Wilson
Affiliations
  • 1. Department of Medicinal Chemistry, Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. [email protected]
PMID: 18621524 DOI: 10.1016/j.bmcl.2008.06.070
Abstract

Modification of the potent imidazole-based B-Raf Inhibitor SB-590885 resulted in the identification of a series of furan-based derivatives with enhanced CNS penetration. One such compound, SB-699393 (17), was examined in vivo to challenge the hypothesis that selective B-Raf inhibitors may be of value in the treatment of stroke.

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