摘要/Abstract
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.
关键词: 环庚三烯酮衍生物, 七元芳环, 胃癌, 生物活性
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-oxocyclohepta- 1,3,6-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.
Key words: tropone, seven-membered aromatic ring, gastric cancer, bioactivity
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