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

…, L Portland, N Jackson, JJ Liu, F Konzelmann…

Index: Chen, Shaoqing; Chen, Li; Le, Nam T.; Zhao, Chunlin; Sidduri, Achyutharao; Lou, Jian Ping; Michoud, Christophe; Portland, Louis; Jackson, Nicole; Liu, Jin-Jun; Konzelmann, Fred; Chi, Feng; Tovar, Christian; Xiang, Qing; Chen, Yingsi; Wen, Yang; Vassilev, Lyubomir T. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 8 p. 2134 - 2138

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Citation Number: 32

Abstract

A novel series of quinolinyl-methylene-thiazolinones has been identified as potent and selective cyclin-dependent kinase 1 (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.