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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

发表时间:2018-09-14  浏览量:163  下载量:42
全部作者: 徐露玫,张丹,朱锦锦,乔春华
作者单位: 苏州大学药学院
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)的表达与多种人类癌症中的不同炎症因子及免疫现象有关。本研究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。这些研究成果有助于拓宽对含有吲哚环的IDO1抑制剂的认识。
关 键 词: 药物化学;免疫治疗;吲哚胺2,3-双加氧酶1;吲哚衍生物
Title: Design, systhesis and activity evaluation of indole derivatives as indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
Author: XU Lumei, ZHANG Dan, ZHU Jinjin, QIAO Chunhua
Organization: College of Pharmaceutical Sciences, Soochow University
Abstract: In the field of tumor immunotherapy, indoleamine 2,3-dioxygenase 1 (IDO1) expression is associated with different inflammatory factors and immunologic consequences in multiple human cancers. In this study, scaffold hopping strategy was used to design and prepare a new set of 17 indole derivatives. Structural modification includes installation of 3-aminoguanidine moiety, 3-carboxamide moiety and 3-arylthio substituted moiety. Among these compounds, IDO1 enzymatic assay found compounds 7b, 10a, 10b show moderate IDO1 inhibition activity. Furthermore, those findings should be considered in the design of indole-containing IDO1 inhibitors.
Key words: medicinal chemistry; immunotherapy; indoleamine 2,3-dioxygenase 1 (IDO1); indole derivatives
发表期数: 2018年9月第17期
引用格式: 徐露玫,张丹,朱锦锦,等. 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[J]. 中国科技论文在线精品论文,2018,11(17):1742-1751.
 
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