title: Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.
abstract: A novel class of 3,7-diphenyl-4-amino-thieno and furo[3,2-c]pyridine has been designed based on pharmacophore models of ATP competitive kinase inhibitors. Versatile synthetic methods via double Suzuki coupling to explore SAR have been established and potent inhibitors against angiogenetic targets, VEGFR2, Tie-2, and EphB4, have been successfully discovered.
authors.affiliation: GlaxoSmithKline K.K., Tsukuba Research Laboratories, 43, Wadai, Tsukuba 300-4247, Ibaraki, Japan. yasushi.miyazaki@gsk.com
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Miyazaki
authors.forename: Masato
authors.initials: M
authors.lastname: Nakano
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Sato
authors.forename: Anne T
authors.initials: AT
authors.lastname: Truesdale
authors.forename: J Darren
authors.initials: JD
authors.lastname: Stuart
authors.forename: Eldridge N
authors.initials: EN
authors.lastname: Nartey
authors.forename: Kendra E
authors.initials: KE
authors.lastname: Hightower
authors.forename: Laurie
authors.initials: L
authors.lastname: Kane-Carson
mesh_terms: D016475:3T3 Cells; D000255:Adenosine Triphosphate / Q000737:chemistry; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D000818:Animals; D001667:Binding, Competitive; D015195:Drug Design; D005663:Furans / Q000138:chemical synthesis / Q000737:chemistry*; D051379:Mice; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry*; D036224:Receptor, EphB4 / Q000037:antagonists & inhibitors; D042787:Receptor, TIE-2 / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors
chemical_list: D020533:Angiogenesis Inhibitors; D005663:Furans; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D013876:Thiophenes; D000255:Adenosine Triphosphate; D036224:Receptor, EphB4; D042787:Receptor, TIE-2; D040301:Vascular Endothelial Growth Factor Receptor-2