title: Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
abstract: We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.
authors.affiliation: Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. mfrohn@amgen.com
authors.forename: Mike
authors.initials: M
authors.lastname: Frohn
authors.forename: Vellarkad
authors.initials: V
authors.lastname: Viswanadhan
authors.forename: Alexander J
authors.initials: AJ
authors.lastname: Pickrell
authors.forename: Jennifer E
authors.initials: JE
authors.lastname: Golden
authors.forename: Kristine M
authors.initials: KM
authors.lastname: Muller
authors.forename: Roland W
authors.initials: RW
authors.lastname: Bürli
authors.forename: Gloria
authors.initials: G
authors.lastname: Biddlecome
authors.forename: Sean C
authors.initials: SC
authors.lastname: Yoder
authors.forename: Norma
authors.initials: N
authors.lastname: Rogers
authors.forename: Jennifer H
authors.initials: JH
authors.lastname: Dao
authors.forename: Randall
authors.initials: R
authors.lastname: Hungate
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Allen