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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (17), p.5182-5185
Hauptverfasser:	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:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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