title: Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.
abstract: Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds demonstrated nanomolar potency in enzyme and cellular mechanistic assays.
authors.affiliation: GlaxoSmithKline, Oncology R&D, NC 27709, USA. patnaiks@mail.nih.gov
authors.forename: Samarjit
authors.initials: S
authors.lastname: Patnaik
authors.forename: Kirk L
authors.initials: KL
authors.lastname: Stevens
authors.forename: Roseanne
authors.initials: R
authors.lastname: Gerding
authors.forename: Felix
authors.initials: F
authors.lastname: Deanda
authors.forename: J Brad
authors.initials: JB
authors.lastname: Shotwell
authors.forename: Jun
authors.initials: J
authors.lastname: Tang
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Hamajima
authors.forename: Hiroko
authors.initials: H
authors.lastname: Nakamura
authors.forename: M Anthony
authors.initials: MA
authors.lastname: Leesnitzer
authors.forename: Anne M
authors.initials: AM
authors.lastname: Hassell
authors.forename: Lisa M
authors.initials: LM
authors.lastname: Shewchuck
authors.forename: Rakesh
authors.initials: R
authors.lastname: Kumar
authors.forename: Huangshu
authors.initials: H
authors.lastname: Lei
authors.forename: Stanley D
authors.initials: SD
authors.lastname: Chamberlain
mesh_terms: D015195:Drug Design; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017526:Receptor, IGF Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011725:Pyridines; D011758:Pyrroles; D017526:Receptor, IGF Type 1