吲哚类衍生物作为吲哚胺 2,3-双加氧酶1(IDO1)抑制剂的设计合成与活性评价
首发时间:2018-05-22
摘要:在肿瘤免疫治疗领域中,吲哚胺 2,3-双加氧酶1 (Indoleamine 2,3-dioxygenase 1 ,IDO1)的表达和多种人类癌症中不同的炎症因子以及免疫现象有关,最近几年,研究人员通过基于结构修饰和高通量筛选的方法报道了多种包含吲哚环的IDO1抑制剂。这些研究成果有助于对含有吲哚环的IDO1抑制剂的认识。在本课题中,运用骨架跃迁的策略设计合成了一系列吲哚衍生物。通过在吲哚环的β位引入氨基胍、芳酰胺和芳硫基合成17个化合物。IDO1酶抑制活性实验发现化合物7b, 10a, 10b具有一定的IDO1抑制活性。
关键词: 免疫治疗 吲哚胺 2,3-双加氧酶1 吲哚衍生物
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ndole Derivatives as Inhibitors of Indoleamine 2,3-dioxygenase 1 Inhibitors.
Abstract:Indoleamine 2,3-dioxygenase 1(IDO1) expression is associated with different prognosis factors and immunologic consequences in multiple human cancers. In recent years, several class of potent IDO1 inhibitors containing scaffolds of indole have been developed through structure-based design and high throughput screening. Furthermore, those findings should be considered in the design of indole-containing IDO inhibitors. In this study, scaffold hopping strategy was used to design and prepare a new set of 17 indole derivatives. Structural modification including installation of 3-aminoguanidine moiety, 3-carboxamide moiety and 3-arylthio substituented moiety. Among these compound, compounds 7b, 10a, 10b were found to show moderate IDO1 inhibition activity.
Keywords: Immunotherapy indoleamine 2,3-dioxygenase 1(IDO1) indole
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吲哚类衍生物作为吲哚胺 2,3-双加氧酶1(IDO1)抑制剂的设计合成与活性评价
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