Evaluation of indazole-based compounds as a new class of potent KDR/VEGFR-2 inhibitors

被引：21
|
作者：
Bauer, David [1 ]
Whittington, Douglas A. [2 ]
Coxon, Angela [4 ]
Bready, James [4 ]
Harriman, Shawn P. [3 ]
Patel, Vinod F. [1 ]
Polverino, Anthony [5 ]
Harmange, Jean-Christophe [1 ]
机构：
[1] Amgen Inc, Dept Med Chem, Cambridge, MA 02139 USA
[2] Amgen Inc, Dept Mol Struct, Cambridge, MA 02139 USA
[3] Amgen Inc, Dept Pharmacokinet & Drug Metab, Cambridge, MA 02139 USA
[4] Amgen Inc, Dept Oncol Res, Thousand Oaks, CA 91320 USA
[5] Amgen Inc, Dept Oncol Res, Seattle, WA 98119 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 17期
关键词：
KDR inhibitor; VEGFR-2; inhibitor; kinase inhibitor;
D O I：
10.1016/j.bmcl.2008.07.080
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 pro. led to determine their pharmacokinetic properties and evaluated in a VEGF-induced vascular permeability assay. (C) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4844 / 4848
页数：5
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