Design and structure–activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases

The synthesis and SAR of 3-benzimidazol-2-yl-1H-indazole analogs developed as inhibitors of receptor tyrosine kinases (RTK) is reported. 3-Benzimidazol-2-yl-1H-indazole analogs were developed as inhibitors of receptor tyrosine kinases (RTK). The synthesis and SAR of this series is reported.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (13), p.3595-3599
Main Authors: McBride, Christopher M., Renhowe, Paul A., Heise, Carla, Jansen, Johanna M., Lapointe, Gena, Ma, Sylvia, Piñeda, Ramon, Vora, Jayesh, Wiesmann, Marion, Shafer, Cynthia M.
Format: Article
Language:English
Subjects:
Animals
Antineoplastic agents
Basic fibroblast growth factor (bFGF)
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Cell Line, Tumor
Cell Proliferation - drug effects
Crystallography, X-Ray
Dose-Response Relationship, Drug
Drug Design
General aspects
Indazole benzimidazole
Indazoles - chemical synthesis
Indazoles - chemistry
Indazoles - pharmacology
Medical sciences
Mice
Mice, Nude
Models, Molecular
Molecular Structure
Pharmacology. Drug treatments
Platelet derived growth factor (PDGF)
Receptor Protein-Tyrosine Kinases - antagonists & inhibitors
Receptor tyrosine kinase (RTK)
Stereoisomerism
Structure-Activity Relationship
Vascular endothelial growth factor (VEGF)
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Description
Summary:The synthesis and SAR of 3-benzimidazol-2-yl-1H-indazole analogs developed as inhibitors of receptor tyrosine kinases (RTK) is reported. 3-Benzimidazol-2-yl-1H-indazole analogs were developed as inhibitors of receptor tyrosine kinases (RTK). The synthesis and SAR of this series is reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.03.069