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Development of a series of novel o-phenylenediamine-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-01-11 , DOI: 10.1016/j.bmcl.2018.01.010 David K Williams 1 , Jay A Markwalder 1 , Aaron J Balog 1 , Bin Chen 1 , Libing Chen 1 , Jennifer Donnell 1 , Lauren Haque 1 , Amy C Hart 1 , Sunil K Mandal 2 , Andrew Nation 1 , Weifang Shan 1 , Gregory D Vite 1 , Kelly Covello 3 , John T Hunt 3 , Maria N Jure-Kunkel 4 , Steven P Seitz 1
中文翻译：
开发一系列基于邻苯二胺的新型吲哚胺 2,3-双加氧酶 1 (IDO1) 抑制剂
更新日期：2018-01-11
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-01-11 , DOI: 10.1016/j.bmcl.2018.01.010 David K Williams 1 , Jay A Markwalder 1 , Aaron J Balog 1 , Bin Chen 1 , Libing Chen 1 , Jennifer Donnell 1 , Lauren Haque 1 , Amy C Hart 1 , Sunil K Mandal 2 , Andrew Nation 1 , Weifang Shan 1 , Gregory D Vite 1 , Kelly Covello 3 , John T Hunt 3 , Maria N Jure-Kunkel 4 , Steven P Seitz 1
Affiliation
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A novel series of o-phenylenediamine-based inhibitors of indoleamine 2,3-dioxygenase (IDO) has been identified. IDO is a heme-containing enzyme, overexpressed in the tumor microenvironment of many cancers, which can contribute to the suppression of the host immune system. Synthetic modifications to a previously described diarylether series resulted in an additional degree of molecular diversity which was exploited to afford compounds that demonstrated significant potency in the HeLa human cervical cancer IDO1 assay.
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中文翻译：
开发一系列基于邻苯二胺的新型吲哚胺 2,3-双加氧酶 1 (IDO1) 抑制剂
已经鉴定了一系列新的基于邻苯二胺的吲哚胺 2,3-双加氧酶 (IDO) 抑制剂。IDO 是一种含血红素的酶，在许多癌症的肿瘤微环境中过度表达，有助于抑制宿主免疫系统。对先前描述的二芳基醚系列的合成修饰导致了额外程度的分子多样性，该多样性被用来提供在 HeLa 人类宫颈癌 IDO1 测定中显示出显着效力的化合物。
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