Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors

被引：54

作者：

Chen, Shaoqing ^{[1
]}

Chen, Li ^{[1
]}

Le, Nam T. ^{[1
]}

Zhao, Chunlin ^{[1
]}

Sidduri, Achyutharao ^{[1
]}

Lou, Jian Ping ^{[1
]}

Michoud, Christophe ^{[1
]}

Portland, Louis ^{[1
]}

Jackson, Nicole ^{[1
]}

Liu, Jin-Jun ^{[1
]}

Konzelmann, Fred ^{[1
]}

Chi, Feng ^{[1
]}

Tovar, Christian ^{[1
]}

Xiang, Qing ^{[1
]}

Chen, Yingsi ^{[1
]}

Wen, Yang ^{[1
]}

Vassilev, Lyubomir T. ^{[1
]}

机构：

[1] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期

关键词：

cyclin-dependent kinase; CDK1; inhibitor; anticancer; CLINICAL DEVELOPMENT; CDK INHIBITORS; CANCER; DISCOVERY; PROGRESS; R547; MICE;

D O I：

10.1016/j.bmcl.2007.01.081

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase I (CDK1) inhibitors. Their synthesis and structure activity relationships (SAR) are described. Representative compounds from this class reversibly inhibit CDK1 activity in vitro, and block cell cycle progression in human tumor cell lines, suggesting a potential use as antitumor agents. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2134 / 2138

页数：5

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