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

…, DK Dean, A Gaiba, EA Irving, FD King, A Naylor…

Index: Takle, Andrew K.; Bamford, Mark J.; Davies, Susannah; Davis, Robert P.; Dean, David K.; Gaiba, Alessandra; Irving, Elaine A.; King, Frank D.; Naylor, Antoinette; Parr, Christopher A.; Ray, Alison M.; Reith, Alastair D.; Smith, Beverley B.; Staton, Penelope C.; Steadman, Jon G.A.; Stean, Tania O.; Wilson, David M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 15 p. 4373 - 4376

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Citation Number: 23

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.