title: Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.
abstract: 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.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, LLC, 1000 Route 202, Raritan, NJ 08869, USA. shenlinhuang@htomail.com
authors.forename: Shenlin
authors.initials: S
authors.lastname: Huang
authors.forename: Ronghua
authors.initials: R
authors.lastname: Li
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: Stuart
authors.initials: S
authors.lastname: Emanuel
authors.forename: Steven A
authors.initials: SA
authors.lastname: Middleton
mesh_terms: 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
chemical_list: D001372:Aza Compounds; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D016203:CDC2 Protein Kinase