Bauer David, Whittington Douglas A, Coxon Angela, Bready James, Harriman Shawn P, Patel Vinod F, Polverino Anthony, Harmange Jean-Christophe
Department of Medicinal Chemistry, Amgen, Inc., One Kendall Square, Building 1000, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett. 2008 Sep 1;18(17):4844-8. doi: 10.1016/j.bmcl.2008.07.080. Epub 2008 Jul 24.
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.
报道了一类新型的、具有强效和选择性的KDR抑制剂，其包含吲唑部分1。已对该系列抑制剂的发现、合成及构效关系进行了研究。还对最有前景的化合物进行了分析以确定其药代动力学性质，并在VEGF诱导的血管通透性试验中进行了评估。
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