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

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2134-8. doi: 10.1016/j.bmcl.2007.01.081.
Shaoqing Chen  1 ,  Li Chen ,  Nam T Le ,  Chunlin Zhao ,  Achyutharao Sidduri ,  Jian Ping Lou ,  Christophe Michoud ,  Louis Portland ,  Nicole Jackson ,  Jin-Jun Liu ,  Fred Konzelmann ,  Feng Chi ,  Christian Tovar ,  Qing Xiang ,  Yingsi Chen ,  Yang Wen ,  Lyubomir T Vassilev
Affiliations
  • 1. Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. [email protected]
PMID: 17303421 DOI: 10.1016/j.bmcl.2007.01.081
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.