Discovery of a potent and selective Aurora kinase inhibitor

被引：101

作者：

Oslob, Johan D. ^{[1
]}

Romanowski, Michael J. ^{[1
]}

Allen, Darin A. ^{[1
]}

Baskaran, Subramanian ^{[1
]}

Bui, Minna ^{[1
]}

Elling, Robert A. ^{[1
]}

Flanagan, William M. ^{[1
]}

Fung, Amy D. ^{[1
]}

Hanan, Emily J. ^{[1
]}

Harris, Shannon ^{[1
]}

Heumann, Stacey A. ^{[1
]}

Hoch, Ute ^{[1
]}

Jacobs, Jeffrey W. ^{[1
]}

Lam, Joni ^{[1
]}

Lawrence, Chris E. ^{[1
]}

McDowell, Robert S. ^{[1
]}

Nannini, Michelle A. ^{[1
]}

Shen, Wang ^{[1
]}

Silverman, Jeffrey A. ^{[1
]}

Sopko, Michelle M. ^{[1
]}

Tangonan, Bradley T. ^{[1
]}

Teague, Juli ^{[1
]}

Yoburn, Josh C. ^{[1
]}

Yu, Chul H. ^{[1
]}

Zhong, Min ^{[1
]}

Zimmerman, Kristin M. ^{[1
]}

O'Brien, Tom ^{[1
]}

Lew, Willard ^{[1
]}

机构：

[1] Sunesis Pharmaceut, Med Chem, San Francisco, CA 94080 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 17期

关键词：

Aurora; kinases; inhibitor; SNS-314;

D O I：

10.1016/j.bmcl.2008.07.073

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This communication describes the discovery of a novel series of Aurora kinase inhibitors. Key SAR and critical binding elements are discussed. Some of the more advanced analogues potently inhibit cellular proliferation and induce phenotypes consistent with Aurora kinase inhibition. In particular, compound 21 (SNS-314) is a potent and selective Aurora kinase inhibitor that exhibits significant activity in pre-clinical in vivo tumor models. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4880 / 4884

页数：5

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