基于结构导向设计取代氮杂苯并咪唑作为有效的缺氧诱导因子-1α脯氨酰羟化酶-2抑制剂
Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
作者信息
Frohn Mike, Viswanadhan Vellarkad, Pickrell Alexander J, Golden Jennifer E, Muller Kristine M, Bürli Roland W, Biddlecome Gloria, Yoder Sean C, Rogers Norma, Dao Jennifer H, Hungate Randall, Allen Jennifer R
机构信息
Department of Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA.
出版信息
Bioorg Med Chem Lett. 2008 Sep 15;18(18):5023-6. doi: 10.1016/j.bmcl.2008.08.012. Epub 2008 Aug 9.
PMID:18755588
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.
摘要
我们报道了一系列基于结构设计与合成的新型氮杂苯并咪唑类化合物作为脯氨酰羟化酶2（PHD2）抑制剂。这些研究成果产生了化合物22，其在体外对PHD2功能表现出高效抑制作用。
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