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

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

Mike Frohn  1 , Vellarkad Viswanadhan, Alexander J Pickrell, Jennifer E Golden, Kristine M Muller, Roland W Bürli, Gloria Biddlecome, Sean C Yoder, Norma Rogers, Jennifer H Dao, Randall Hungate, Jennifer R Allen
Affiliations

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

Mike Frohn et al. Bioorg Med Chem Lett. .

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.

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