title: Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
abstract: Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase.
authors.affiliation: Department of Medicinal Chemistry, Amgen Inc., One Kendall Square, Bldg. 1000, Cambridge, MA 02139, USA. vcee@amgen.com
authors.forename: Victor J
authors.initials: VJ
authors.lastname: Cee
authors.forename: Alan C
authors.initials: AC
authors.lastname: Cheng
authors.forename: Karina
authors.initials: K
authors.lastname: Romero
authors.forename: Steve
authors.initials: S
authors.lastname: Bellon
authors.forename: Christopher
authors.initials: C
authors.lastname: Mohr
authors.forename: Douglas A
authors.initials: DA
authors.lastname: Whittington
authors.forename: Annette
authors.initials: A
authors.lastname: Bak
authors.forename: James
authors.initials: J
authors.lastname: Bready
authors.forename: Sean
authors.initials: S
authors.lastname: Caenepeel
authors.forename: Angela
authors.initials: A
authors.lastname: Coxon
authors.forename: Holly L
authors.initials: HL
authors.lastname: Deak
authors.forename: Jenne
authors.initials: J
authors.lastname: Fretland
authors.forename: Yan
authors.initials: Y
authors.lastname: Gu
authors.forename: Brian L
authors.initials: BL
authors.lastname: Hodous
authors.forename: Xin
authors.initials: X
authors.lastname: Huang
authors.forename: Joseph L
authors.initials: JL
authors.lastname: Kim
authors.forename: Jasmine
authors.initials: J
authors.lastname: Lin
authors.forename: Alexander M
authors.initials: AM
authors.lastname: Long
authors.forename: Hanh
authors.initials: H
authors.lastname: Nguyen
authors.forename: Philip R
authors.initials: PR
authors.lastname: Olivieri
authors.forename: Vinod F
authors.initials: VF
authors.lastname: Patel
authors.forename: Ling
authors.initials: L
authors.lastname: Wang
authors.forename: Yihong
authors.initials: Y
authors.lastname: Zhou
authors.forename: Paul
authors.initials: P
authors.lastname: Hughes
authors.forename: Stephanie
authors.initials: S
authors.lastname: Geuns-Meyer
mesh_terms: D000284:Administration, Oral; D001562:Benzimidazoles / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D001682:Biological Availability; D018360:Crystallography, X-Ray; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D042787:Receptor, TIE-2 / Q000037:antagonists & inhibitors*
chemical_list: D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D042787:Receptor, TIE-2