The identification of potent and selective imidazole-based inhibitors of B-Raf kinase

Andrew K Takle; Murray J B Brown; Susannah Davies; David K Dean; Gerraint Francis; Alessandra Gaiba; Alex W Hird; Frank D King; Peter J Lovell; Antoinette Naylor; Alastair D Reith; Jon G Steadman; David M Wilson

doi:10.1016/j.bmcl.2005.09.072

The identification of potent and selective imidazole-based inhibitors of B-Raf kinase

Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81. doi: 10.1016/j.bmcl.2005.09.072. Epub 2005 Nov 2.

Authors

Andrew K Takle¹, Murray J B Brown, Susannah Davies, David K Dean, Gerraint Francis, Alessandra Gaiba, Alex W Hird, Frank D King, Peter J Lovell, Antoinette Naylor, Alastair D Reith, Jon G Steadman, David M Wilson

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: 16260133
DOI: 10.1016/j.bmcl.2005.09.072

Abstract

A novel triarylimidazole derivative, SB-590885 (33), bearing a 2,3-dihydro-1H-inden-1-one oxime substituent has been identified as a potent and extremely selective inhibitor of B-Raf kinase.

MeSH terms

Cyclization
Imidazoles / chemical synthesis
Imidazoles / chemistry
Imidazoles / pharmacology*
Molecular Structure
Proto-Oncogene Proteins B-raf / antagonists & inhibitors*
Proto-Oncogene Proteins B-raf / chemistry
Structure-Activity Relationship

Substances

Imidazoles
SB-590885
Proto-Oncogene Proteins B-raf