title: Pyridinylimidazole inhibitors of Tie2 kinase.
abstract: This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOPC-315 plasmacytoma xenograft model.
authors.affiliation: GlaxoSmithKline, Collegeville, PA 19426, USA. marcus.a.semones@gsk.com
authors.forename: Marcus
authors.initials: M
authors.lastname: Semones
authors.forename: Yanhong
authors.initials: Y
authors.lastname: Feng
authors.forename: Neil
authors.initials: N
authors.lastname: Johnson
authors.forename: Jerry L
authors.initials: JL
authors.lastname: Adams
authors.forename: Jim
authors.initials: J
authors.lastname: Winkler
authors.forename: Michael
authors.initials: M
authors.lastname: Hansbury
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D008958:Models, Molecular; D009368:Neoplasm Transplantation; D010954:Plasmacytoma / Q000188:drug therapy*; D011725:Pyridines / Q000494:pharmacology; D042787:Receptor, TIE-2 / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D048051:p38 Mitogen-Activated Protein Kinases / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D007093:Imidazoles; D011725:Pyridines; D042787:Receptor, TIE-2; D048051:p38 Mitogen-Activated Protein Kinases; C093642:SB 203580