Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
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.
Frohn
Mike
M
Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. mfrohn@amgen.com
Viswanadhan
Vellarkad
V
Pickrell
Alexander J
AJ
Golden
Jennifer E
JE
Muller
Kristine M
KM
Bürli
Roland W
RW
Biddlecome
Gloria
G
Yoder
Sean C
SC
Rogers
Norma
N
Dao
Jennifer H
JH
Hungate
Randall
R
Allen
Jennifer R
JR