title: Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.
abstract: Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure-activity relationships against IGF-1R kinase activity as well as inhibition of the hERG ion channel are discussed.
authors.affiliation: AstraZeneca, Oncology Innovative Medicines, Centre de recherches, Z.I. Pompelle, 51689 Reims Cedex 2, France. richard.ducray@astrazeneca.com
authors.forename: Richard
authors.initials: R
authors.lastname: Ducray
authors.forename: Clifford D
authors.initials: CD
authors.lastname: Jones
authors.forename: Frederic H
authors.initials: FH
authors.lastname: Jung
authors.forename: Iain
authors.initials: I
authors.lastname: Simpson
authors.forename: Jon
authors.initials: J
authors.lastname: Curwen
authors.forename: Martin
authors.initials: M
authors.lastname: Pass
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D055808:Drug Discovery; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors; D006801:Humans; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000814:Aniline Compounds; D051638:Ether-A-Go-Go Potassium Channels; D047428:Protein Kinase Inhibitors; D011725:Pyridines; D017526:Receptor, IGF Type 1; C001439:imidazo(1,2-a)pyridine; C023650:aniline