Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Stellwagen, JC; Adjabeng, GM; Arnone, MR; Dickerson, SH; Han, C; Hornberger, KR; King, AJ; Mook, RA; Petrov, KG; Rheault, TR; Rominger, CM; Rossanese, OW; Smitheman, KN; Waterson, AG; Uehling, DE

Published Date

  • August 1, 2011

Published In

Volume / Issue

  • 21 / 15

Start / End Page

  • 4436 - 4440

PubMed ID

  • 21733693

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2011.06.021


  • eng

Conference Location

  • England