title: Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
abstract: The novel compound 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine was discovered to be a potent CDK1 inhibitor. Described here is the chemistry for its synthesis, including Pd(II) catalyzed Stille coupling reaction and sulfur(0) induced benzimidazole formation. Its effects on VEGFR-2 kinase activity and tumour cell proliferation are also described.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development L. L. C., 1000 Route 202, Raritan, NJ 08869, USA. shenlinhuang@hotmail.com
authors.forename: Shenlin
authors.initials: S
authors.lastname: Huang
authors.forename: Ronghui
authors.initials: R
authors.lastname: Lin
authors.forename: Yang
authors.initials: Y
authors.lastname: Yu
authors.forename: Yanhua
authors.initials: Y
authors.lastname: Lu
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: George
authors.initials: G
authors.lastname: Chiu
authors.forename: Shengjian
authors.initials: S
authors.lastname: Li
authors.forename: Stuart L
authors.initials: SL
authors.lastname: Emanuel
authors.forename: Steven A
authors.initials: SA
authors.lastname: Middleton
mesh_terms: D001562:Benzimidazoles; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors*; D002384:Catalysis; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007546:Isoquinolines / Q000138:chemical synthesis / Q000494:pharmacology; D010165:Palladium; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013455:Sulfur; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000187:drug effects
chemical_list: C519550:3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo(1,2-b)pyridine; D001562:Benzimidazoles; D007546:Isoquinolines; D011725:Pyridines; D010165:Palladium; D013455:Sulfur; C031000:benzimidazole; D040301:Vascular Endothelial Growth Factor Receptor-2; D016203:CDC2 Protein Kinase