含吲哚的α-氨基膦酸酯衍生物的合成及抗肿瘤活性研究

发布时间：2018-06-26 04:57

本文选题：吲哚 + α-氨基膦酸酯　；参考：《郑州大学》2014年硕士论文

【摘要】：吲哚是一类重要的含氮杂环化合物，有着多种生物、药物活性，其衍生物具有良好的抗菌，抗炎，抗肿瘤，抗疟疾，抗病毒，抗HIV，抗氧化，杀虫，抗惊厥等生物活性，而被广泛应用于农药，医药，染料，香料等领域，因此倍受关注。而α-氨基膦酸酯类化合物，，也由于其具有多种生物活性而被广泛应用于医药，农药行业。基于吲哚类和α-氨基膦酸酯类化合物均有多种生物活性，我们将吲哚环和α-氨基膦酸酯设计在同一个分子中，共合成得到了22个未见文献报道的含吲哚和α-氨基膦酸酯的新型化合物(7A1~7A8、7B1~7B8、7C1~7C6)。所有目标化合物的结构经1H NMR、13C NMR、31P NMR、IR、MS和HRMS确认，其中A2、B1和C3经X-单晶衍射进一步确证结构。同时测定了化合物对人类肝癌细胞(HepG2)、人类胃癌细胞(MGC803)和人类食道癌细胞(EC109)三种癌细胞的抑制活性。合成路线如Scheme1所示。Scheme1目标化合物的合成路线
[Abstract]:Indole is an important class of nitrogen-containing heterocyclic compounds, with a variety of biological, drug activity, its derivatives have good antibacterial, anti-inflammatory, anti-tumor, anti-malaria, anti-virus, anti-HIV, anti-oxidation, insecticidal, anti-convulsion and other biological activities. And widely used in pesticide, medicine, dyes, spices and other fields, so much attention. And 伪-aminophosphonic acid esters are widely used in medicine and pesticide industry because of their various biological activities. Based on the fact that indoles and 伪 -aminophosphonic acid esters have a variety of biological activities, we designed indole-ring and 伪 -aminophosphonic acid esters in the same molecule. A total of 22 new compounds containing indoles and 伪 -aminophosphonates (7A _ 1O _ 7A _ (8) B _ (1) O _ (7B _ (8) C _ (1) C _ (1) C _ (6) have been synthesized. The structures of all the target compounds were confirmed by 1H-NMR-13C NMR-31P NMR-IRMS and HRMS, and the structures of A2B1-and C3 were further confirmed by X-ray diffraction. At the same time, the inhibitory activity of the compounds on human hepatoma cells (HepG2), human gastric cancer cells (MGC803) and human esophageal cancer cells (EC109) was determined. The synthetic route of a target compound, as shown in Scheme1.
【学位授予单位】：郑州大学
【学位级别】：硕士
【学位授予年份】：2014
【分类号】：R914;O626

【二级参考文献】