Aza-stilbenes as potent and selective c-RAF inhibitors

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. The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RA...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (20), p.5378-5383
Main Authors: McDonald, Octerloney, Lackey, Karen, Davis-Ward, Ronda, Wood, Edgar, Samano, Vicente, Maloney, Patrick, Deanda, Felix, Hunter, Robert
Format: Article
Language:English
Subjects:
Antineoplastic agents
Aza Compounds - chemical synthesis
Aza Compounds - chemistry
Aza Compounds - pharmacology
Aza-stilbene
Binding Sites
Biological and medical sciences
c-RAF
Enzyme Activation - drug effects
General aspects
Kinase
Medical sciences
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Protein Conformation
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Proto-Oncogene Proteins c-raf - antagonists & inhibitors
Stereoisomerism
Stilbenes - chemical synthesis
Stilbenes - chemistry
Stilbenes - pharmacology
Structure-Activity Relationship
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.07.063