Discovery of highly potent and selective type I B-Raf kinase inhibitors

A series of pyrazolo[1,5-α]pyrimidine analogs has been prepared and found to be extremely potent and selective B-Raf inhibitors. A series of pyrazolo[1,5-α]pyrimidine analogs has been prepared and found to be potent and selective B-Raf inhibitors. Molecular modeling suggests they bind to the active...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-12, Vol.19 (23), p.6571-6574
Main Authors: Wang, Xiaolun, Berger, Dan M., Salaski, Edward J., Torres, Nancy, Hu, Yongbo, Levin, Jeremy I., Powell, Dennis, Wojciechowicz, Donald, Collins, Karen, Frommer, Eileen
Format: Article
Language:English
Subjects:
Antineoplastic agents
B-Raf
Biological and medical sciences
Drug Discovery
General aspects
Inhibitors
Kinase
Medical sciences
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Protein Kinase Inhibitors - chemical synthesis
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - pharmacology
Proto-Oncogene Proteins B-raf - antagonists & inhibitors
Proto-Oncogene Proteins B-raf - metabolism
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - pharmacology
Raf
RAS
Structure-Activity Relationship
Substrate Specificity
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Summary:A series of pyrazolo[1,5-α]pyrimidine analogs has been prepared and found to be extremely potent and selective B-Raf inhibitors. A series of pyrazolo[1,5-α]pyrimidine analogs has been prepared and found to be potent and selective B-Raf inhibitors. Molecular modeling suggests they bind to the active conformation of the enzyme.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.10.030