Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors

A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure−activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.

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Bibliographic Details
Published in:Journal of medicinal chemistry 2008-11, Vol.51 (22), p.7049-7052
Main Authors: Ramurthy, Savithri, Subramanian, Sharadha, Aikawa, Mina, Amiri, Payman, Costales, Abran, Dove, Jeff, Fong, Susan, Jansen, Johanna M, Levine, Barry, Ma, Sylvia, McBride, Christopher M, Michaelian, Jonah, Pick, Teresa, Poon, Daniel J, Girish, Sandhya, Shafer, Cynthia M, Stuart, Darrin, Sung, Leonard, Renhowe, Paul A
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Antineoplastic agents
Benzimidazoles - administration & dosage
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Biological Availability
Cell Line, Tumor
Cell Proliferation - drug effects
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug Design
Female
General aspects
Humans
Medical sciences
Mice
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Protein Kinase Inhibitors - administration & dosage
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Protein Structure, Tertiary
raf Kinases - antagonists & inhibitors
raf Kinases - metabolism
Stereoisomerism
Structure-Activity Relationship
Xenograft Model Antitumor Assays
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Description
Summary:A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure−activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm801050k