Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors

A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (17), p.5182-5185
Main Authors: Patel, Hitesh K., Grotzfeld, Robert M., Lai, Andiliy G., Mehta, Shamal A., Milanov, Zdravko V., Chao, Qi, Sprankle, Kelly G., Carter, Todd A., Velasco, Anne Marie, Fabian, Miles A., James, Joyce, Treiber, Daniel K., Lockhart, David J., Zarrinkar, Patrick P., Bhagwat, Shripad S.
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacokinetics
Biological and medical sciences
Cell Line, Tumor
FLT3
fms-Like Tyrosine Kinase 3 - antagonists & inhibitors
fms-Like Tyrosine Kinase 3 - metabolism
General aspects
Humans
Kinase inhibitor
Medical sciences
Mice
Mice, Nude
Miscellaneous
Pharmacology. Drug treatments
Potent
Selective
Structure-Activity Relationship
Urea - analogs & derivatives
Urea - chemical synthesis
Urea - pharmacokinetics
Xenograft Model Antitumor Assays
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Description
Summary:A series of diaryl ureas with an amide substitution at the 4-position was prepared and found to be potent and selective FLT3 inhibitors with good oral bioavailability and efficacy in a tumor xenograft model.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.07.024