title: Aza-stilbenes as potent and selective c-RAF inhibitors.
abstract: The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A hypothesis for the binding mode, activity, and selectivity is proposed.
authors.affiliation: GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
authors.forename: Octerloney
authors.initials: O
authors.lastname: McDonald
authors.forename: Karen
authors.initials: K
authors.lastname: Lackey
authors.forename: Ronda
authors.initials: R
authors.lastname: Davis-Ward
authors.forename: Edgar
authors.initials: E
authors.lastname: Wood
authors.forename: Vicente
authors.initials: V
authors.lastname: Samano
authors.forename: Patrick
authors.initials: P
authors.lastname: Maloney
authors.forename: Felix
authors.initials: F
authors.lastname: Deanda
authors.forename: Robert
authors.initials: R
authors.lastname: Hunter
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D004789:Enzyme Activation / Q000187:drug effects; D008958:Models, Molecular; D015394:Molecular Structure; D011487:Protein Conformation; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019908:Proto-Oncogene Proteins c-raf / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D001372:Aza Compounds; D047428:Protein Kinase Inhibitors; D013267:Stilbenes; D019908:Proto-Oncogene Proteins c-raf