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.

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收藏

页码：4844 / 4848

页数：5

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