2. Academic Validation
  3. Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup

  • Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021.
John C Stellwagen 1,  George M Adjabeng,  Marc R Arnone,  Scott H Dickerson,  Chao Han,  Keith R Hornberger,  Alastair J King,  Robert A Mook Jr,  Kimberly G Petrov,  Tara R Rheault,  Cynthia M Rominger,  Olivia W Rossanese,  Kimberly N Smitheman,  Alex G Waterson,  David E Uehling
Affiliations

Affiliation

  • 1 GlaxoSmithKline Oncology CEDD, Research Triangle Park, NC 27709-3398, United States. john.stellwagen@amgen.com
PMID: 21733693 DOI: 10.1016/j.bmcl.2011.06.021
Abstract

A potent series of inhibitors against the B-Raf(V600E) kinase have been developed that show excellent activity in cellular assays and good oral bioavailability in rats. The key structural features of the series are an arylsulfonamide headgroup, a thiazole core, and a fluorine ortho to the sulfonamide nitrogen.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-120676
    B-Raf抑制剂
    Raf
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