2. Academic Validation
  3. 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
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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