title: Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.
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.
authors.affiliation: Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. shaoqing.chen@roche.com
authors.forename: Shaoqing
authors.initials: S
authors.lastname: Chen
authors.forename: Li
authors.initials: L
authors.lastname: Chen
authors.forename: Nam T
authors.initials: NT
authors.lastname: Le
authors.forename: Chunlin
authors.initials: C
authors.lastname: Zhao
authors.forename: Achyutharao
authors.initials: A
authors.lastname: Sidduri
authors.forename: Jian Ping
authors.initials: JP
authors.lastname: Lou
authors.forename: Christophe
authors.initials: C
authors.lastname: Michoud
authors.forename: Louis
authors.initials: L
authors.lastname: Portland
authors.forename: Nicole
authors.initials: N
authors.lastname: Jackson
authors.forename: Jin-Jun
authors.initials: JJ
authors.lastname: Liu
authors.forename: Fred
authors.initials: F
authors.lastname: Konzelmann
authors.forename: Feng
authors.initials: F
authors.lastname: Chi
authors.forename: Christian
authors.initials: C
authors.lastname: Tovar
authors.forename: Qing
authors.initials: Q
authors.lastname: Xiang
authors.forename: Yingsi
authors.initials: Y
authors.lastname: Chen
authors.forename: Yang
authors.initials: Y
authors.lastname: Wen
authors.forename: Lyubomir T
authors.initials: LT
authors.lastname: Vassilev
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D013844:Thiazoles; D016203:CDC2 Protein Kinase