1. Academic Validation
  2. The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase

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

Affiliation

  • 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. Andy.K.Takle@gsk.com
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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