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Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors |
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| Authors: | Bauer David Whittington Douglas A Coxon Angela Bready James Harriman Shawn P Patel Vinod F Polverino Anthony Harmange Jean-Christophe |
| Institution: | Department of Medicinal Chemistry, Amgen, Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA. |
| Abstract: | A novel class of potent and selective inhibitors of KDR incorporating an indazole moiety 1 is reported. The discovery, synthesis, and structure–activity relationships of this series of inhibitors have been investigated. The most promising compounds were also profiled to determine their pharmacokinetic properties and evaluated in a VEGF-induced vascular permeability assay. |
| Keywords: | KDR inhibitor VEGFR-2 inhibitor Kinase inhibitor |
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