Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.
A novel series of 2-amino-4-(7-azaindol-3-yl)pyrimidines was discovered as cyclin dependent kinase 1 (CDK1) inhibitors. The core structure was synthesized via Pd(II) catalyzed coupling reaction. A number of analogues showed good potency for CDK1 and exhibited cellular antiproliferation activity. The structure-activity relationship is described.
Huang
Shenlin
S
Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA. shenlinhuang@htomail.com
Li
Ronghua
R
Connolly
Peter J
PJ
Emanuel
Stuart
S
Middleton
Steven A
SA
D000586:Amination; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D001372:Aza Compounds; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D016203:CDC2 Protein Kinase