title: Aminofurazans as potent inhibitors of AKT kinase.
abstract: AKT inhibitors containing an imidazopyridine aminofurazan scaffold have been optimized. We have previously disclosed identification of the AKT inhibitor GSK690693, which has been evaluated in clinical trials in cancer patients. Herein we describe recent efforts focusing on investigating a distinct region of this scaffold that have afforded compounds (30 and 32) with comparable activity profiles to that of GSK690693.
authors.affiliation: Oncology Chemistry, GlaxoSmithKline, Collegeville, PA 19426, USA.
authors.forename: Meagan B
authors.initials: MB
authors.lastname: Rouse
authors.forename: Mark A
authors.initials: MA
authors.lastname: Seefeld
authors.forename: Jack D
authors.initials: JD
authors.lastname: Leber
authors.forename: Kenneth C
authors.initials: KC
authors.lastname: McNulty
authors.forename: Lihui
authors.initials: L
authors.lastname: Sun
authors.forename: William H
authors.initials: WH
authors.lastname: Miller
authors.forename: Shuyun
authors.initials: S
authors.lastname: Zhang
authors.forename: Elisabeth A
authors.initials: EA
authors.lastname: Minthorn
authors.forename: Nestor O
authors.initials: NO
authors.lastname: Concha
authors.forename: Anthony E
authors.initials: AE
authors.lastname: Choudhry
authors.forename: Michael D
authors.initials: MD
authors.lastname: Schaber
authors.forename: Dirk A
authors.initials: DA
authors.lastname: Heerding
mesh_terms: D000818:Animals; D002460:Cell Line; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D006801:Humans; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D017433:Protein Structure, Secondary / Q000502:physiology; D051057:Proto-Oncogene Proteins c-akt / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C528328:GSK690693; D010069:Oxadiazoles; D047428:Protein Kinase Inhibitors; D051057:Proto-Oncogene Proteins c-akt