环庚三烯酮衍生物的合成和抑制胃癌细胞增殖的活性研究  

Synthesis and Bioactivity of Tropone Derivatives as Potential Compounds against Human Gastric Cancer Cells Growth

作　　者：邵继炎 李志杰 王迓君 熊裕焱 胡向东[1] Shao Jiyan;a Li Zhijie;Wang Yajun;Xiong Yuyan;Hu Xiangdong(Key Laboratory of Synthetic and National Functional Molecule Chemistry of Ministry of Education,College of Chemistry&Materials Science,Northwest University,Xi'an 710127;Key Laboratory of Resource Biology and Biotechnology in Western China,Ministry of Education,School of Medicine,Northwest University,Xi'an 710069)

机构地区：[1]西北大学化学与材料科学学院合成与天然功能分子教育部重点实验室,西安710127 [2]西北大学医学院西部资源生物与现代生物技术教育部重点实验室,西安710069

出　　处：《有机化学》2021年第9期3675-3681,共7页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.21772153,22071192);陕西省科技厅基金(No.2019JM-151);陕西省科技创新团队(No.2017KCT-37);陕西省自然科学基金(No.2020JQ-611);陕西省教育厅2020年突发公共卫生安全专项科学研究计划(No.20JG034);陕西省高层次人才资助项目.

摘　　要：基于已知的金催化氧化六元环扩环策略,实现了一系列环庚三烯酮衍生物的合成.发现环庚三烯酮衍生物2-羟基-3,6-二甲基-5-氧代-1,3,6-环庚三烯-1-羧酸乙酯(3)、3,6-二甲基-7-氧代-4-((三氟甲基)磺酰基)氧基-1,3,5-环庚三烯-1-羧酸乙酯(9)、3,6-二甲基-7-氧代-4-乙烯基-1,3,5-环庚三烯-1-羧酸乙酯(10)人胃癌细胞MGC-27表现出抗增殖活性,而活性相对较好的化合物9的抗增殖活性与胃癌细胞MGC-27凋亡没有关联.Based on the strategy of Au-catalyzed oxidative ring expansion of six-membered rings,the synthesis of a series of tropone derivatives was achieved.It was disclosed that tropone derivatives ethyl 2-hydroxy-3,6-dimethyl-5-oxocyclohepta1,3,6-triene-1-carboxylate(3),ethyl 3,6-dimethyl-7-oxo-4-(((trifluoromethyl)sulfonyl)oxy)cyclohepta-1,3,5-triene-1-carboxylate(9),and ethyl 3,6-dimethyl-7-oxo-4-vinylcyclohepta-1,3,5-triene-1-carboxylate(10)displayed antiproliferative activity against human gastric cancer cells MGC-27.Compound 9,which possesses relatively better activity,didn’t show relationship between its antiproliferative activity and the apoptosis of gastric cancer cells MGC-27.

关 键 词：环庚三烯酮衍生物 七元芳环 胃癌 生物活性 

分 类 号：TQ460.1[化学工程—制药化工]