Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors.
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.
Chen
Shaoqing
S
Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. shaoqing.chen@roche.com
Chen
Li
L
Le
Nam T
NT
Zhao
Chunlin
C
Sidduri
Achyutharao
A
Lou
Jian Ping
JP
Michoud
Christophe
C
Portland
Louis
L
Jackson
Nicole
N
Liu
Jin-Jun
JJ
Konzelmann
Fred
F
Chi
Feng
F
Tovar
Christian
C
Xiang
Qing
Q
Chen
Yingsi
Y
Wen
Yang
Y
Vassilev
Lyubomir T
LT
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
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D013844:Thiazoles; D016203:CDC2 Protein Kinase