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N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Mar 01; Vol. 19 (5), pp. 1323-8. Date of Electronic Publication: 2009 Jan 27. - Publication Year :
- 2009
-
Abstract
- A series of N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting c-Met and VEGFR2 tyrosine kinases was designed and synthesized. The compounds were potent against these two enzymes with IC(50) values in the low nanomolar range in vitro, possessed favorable pharmacokinetic profiles and showed high efficacy in vivo in several human tumor xenograft models in mice.
- Subjects :
- Amides pharmacology
Animals
Cell Line, Tumor
HCT116 Cells
Humans
Imidazolidines pharmacology
Mice
Protein Kinase Inhibitors pharmacology
Rats
Vascular Endothelial Growth Factor Receptor-2 metabolism
Xenograft Model Antitumor Assays methods
Amides chemistry
Imidazolidines chemistry
Protein Kinase Inhibitors chemistry
Proto-Oncogene Proteins c-met administration & dosage
Receptor Protein-Tyrosine Kinases antagonists & inhibitors
Vascular Endothelial Growth Factor Receptor-2 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 19
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 19211249
- Full Text :
- https://doi.org/10.1016/j.bmcl.2009.01.068