新型双（吲哚基）甲烷：具有抗癌特性的 1-羟亚氨基甲基衍生物的从头合成。
Novel approach to bis(indolyl)methanes: de novo synthesis of 1-hydroxyiminomethyl derivatives with anti-cancer properties.
机构信息
Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal; CIQA, FCT, University of Algarve, Campus de Gambelas, 8005-139 Faro, Portugal.
Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.
出版信息
Eur J Med Chem. 2015 Mar 26;93:9-15. doi: 10.1016/j.ejmech.2015.01.050. Epub 2015 Jan 26.
A versatile and broad range approach to previously unknown bis(indolyl)methane oximes based on two consecutive hetero Diels-Alder cycloaddition reactions of electrophilic conjugated nitrosoalkenes with indoles is disclosed. The cytotoxic properties and selectivity of some adducts against several human cancer cell lines pointing to a promising role in the development of anti-tumoural drugs, in particular for leukaemia and lymphoma.
本研究揭示了一种基于亲电硝酮共轭硝基烯与吲哚的两个连续杂 Diels-Alder 环加成反应的多功能、广谱的方法，用于合成以前未知的双（吲哚基）甲烷肟。一些加合物对多种人癌细胞系的细胞毒性和选择性表明其在开发抗肿瘤药物方面具有广阔的前景，特别是在白血病和淋巴瘤方面。
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