Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup

Autor:	Tara Renae Rheault, Kimberly N. Smitheman, Kimberly G. Petrov, Chao Han, George Adjabeng, Alex G. Waterson, Marc R. Arnone, Alastair J. King, David E. Uehling, Olivia W. Rossanese, Keith R. Hornberger, Scott Howard Dickerson, John Stellwagen, Cynthia M. Rominger, Robert A. Mook
Rok vydání:	2011
Předmět:	Proto-Oncogene Proteins B-raf Stereochemistry Clinical Biochemistry Administration Oral Pharmaceutical Science Biochemistry Structure-Activity Relationship chemistry.chemical_compound Catalytic Domain Drug Discovery Animals Thiazole Protein Kinase Inhibitors Molecular Biology chemistry.chemical_classification Sulfonamides Binding Sites Kinase Chemistry Organic Chemistry Fluorine Rats Bioavailability Sulfonamide Amino Acid Substitution Microsomes Liver Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:4436-4440
ISSN:	0960-894X
Popis:	A potent series of inhibitors against the B-RafV600E 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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15c814f8930dd9b7f17ce5a15f5e5352 https://doi.org/10.1016/j.bmcl.2011.06.021 Zobrazit plný text záznamu Full Text from ScienceDirect