Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

被引：51

作者：

Cee, Victor J. ^{[1
]}

Cheng, Alan C. ^{[2
,6
]}

Romero, Karina ^{[1
]}

Bellon, Steve ^{[2
,6
]}

Mohr, Christopher ^{[2
,6
]}

Whittington, Douglas A. ^{[2
,6
]}

Bak, Annette ^{[3
]}

Bready, James ^{[5
]}

Caenepeel, Sean ^{[5
]}

Coxon, Angela ^{[5
]}

Deak, Holly L. ^{[1
]}

Fretland, Jenne ^{[4
,7
]}

Gu, Yan ^{[2
,6
]}

Hodous, Brian L. ^{[1
]}

Huang, Xin ^{[2
,6
]}

Kim, Joseph L. ^{[2
,6
]}

Lin, Jasmine ^{[4
,7
]}

Long, Alexander M. ^{[2
,6
]}

Nguyen, Hanh ^{[1
]}

Olivieri, Philip R. ^{[1
]}

Patel, Vinod F. ^{[1
]}

Wang, Ling ^{[5
]}

Zhou, Yihong ^{[4
,7
]}

Hughes, Paul ^{[5
]}

Geuns-Meyer, Stephanie ^{[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 Pharmaceut, Cambridge, MA 02139 USA

[4] Amgen Inc, Dept Pharmacokinet & Drug Metab, Cambridge, MA 02139 USA

[5] Amgen Inc, Dept Oncol Res, Thousand Oaks, CA 91320 USA

[6] Amgen Inc, Dept Mol Struct, Thousand Oaks, CA 91320 USA

[7] Amgen Inc, Dept Pharmacokinet & Drug Metab, Thousand Oaks, CA 91320 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 02期

关键词：

Tie-2; kinase; Angiogenesis; Kinase inhibitor; Benzimidazole; ANGIOGENESIS; RECEPTORS;

D O I：

10.1016/j.bmcl.2008.11.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：424 / 427

页数：4

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