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Thienopyridine urea inhibitors of KDR kinase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Mar 01; Vol. 17 (5), pp. 1246-9. Date of Electronic Publication: 2006 Dec 09. - Publication Year :
- 2007
-
Abstract
- A series of substituted thienopyridine ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 2, are potent inhibitors of KDR (<10 nM) in both enzymatic and cellular assays. Further characterization of inhibitor 2 indicated that this analog possessed excellent in vivo potency (ED50 2.1 mg/kg) as measured in an estradiol-induced mouse uterine edema model.
- Subjects :
- Animals
Disease Models, Animal
Edema chemically induced
Estradiol
Female
Mice
Models, Molecular
Pyridines pharmacology
Structure-Activity Relationship
Urea chemistry
Urea pharmacology
Uterine Diseases pathology
Pyridines chemical synthesis
Urea chemical synthesis
Vascular Endothelial Growth Factor Receptor-2 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17188869
- Full Text :
- https://doi.org/10.1016/j.bmcl.2006.12.015