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
Language
- eng
Conference Location
- England