Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.

Article Details

Citation

Copy to clipboard

Frohn M, Viswanadhan V, Pickrell AJ, Golden JE, Muller KM, Burli RW, Biddlecome G, Yoder SC, Rogers N, Dao JH, Hungate R, Allen JR

Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5023-6. doi: 10.1016/j.bmcl.2008.08.012. Epub 2008 Aug 9.

PubMed ID

18755588 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
N-[(4-HYDROXY-8-IODOISOQUINOLIN-3-YL)CARBONYL]GLYCINE	Egl nine homolog 1	IC 50 (nM)	1400	N/A	N/A	Details