新型5,6-二氢-6-烷基吡喃酮类衍生物的设计、合成及肿瘤细胞增殖抑制活性研究
发布时间：2019-04-29 13:51
【摘要】：为了研究吡喃酮结构中不饱和双键修饰对该类化合物生物活性的影响.基于5,6-二氢-6-烷基吡喃酮类化合物哥纳香甲素,通过不饱和双键的修饰,设计合成了化合物5,6和8.利用噻唑蓝(MTT)法评价了目标化合物对人肝癌细胞(7721)、人肺癌细胞(A549)、人食管癌细胞(EC-109)、人胃癌细胞(MGC-803)的细胞增殖抑制活性.通过和阳性药物的对比发现,除了4-(2,3,4,5-四氟)苯甲酰氨基-3-甲基-6-苄氧甲基-5,6-二氢-吡喃-2-酮(6d),所合成化合物的肿瘤细胞增殖抑制活性均消失.结果表明,在5,6-二氢-6-烷基吡喃酮类化合物结构中,不饱和双键起着至关重要的作用,对其进行适当的修饰,在保留其活性的同时,具有潜在改善其因共价键结合引起毒性的可能性.
[Abstract]:In order to study the effect of unsaturated double bond modification in pyranone structure on the bioactivity of these compounds. Based on 5,6-dihydro-6-alkyl pyranone compounds, 5, 6 and 8 were designed and synthesized by modification of unsaturated double bonds. The inhibitory effects of the target compounds on human hepatoma cells (7721), human lung cancer cells (A549), human esophageal cancer cells (EC-109) and human gastric cancer cells (MGC-803) were evaluated by thiazole blue (MTT) assay. Compared with the positive drugs, it was found that except 4-(2,3,4,5-tetrafluoro) benzoyl amino-3-methyl-6-benzyloxy methyl-5,6-dihydro-pyran-2-one (6d), The inhibitory activity of the synthesized compounds on the proliferation of tumor cells disappeared. The results show that unsaturated double bonds play an important role in the structure of 5,6-dihydro-6-alkyl pyranones. It has the potential to improve its toxicity due to covalent bond binding.
【作者单位】： 郑州大学药学院;河北北方学院药学系;
【基金】：河南省高校科技创新人才计划(No.14HASTIT0031)资助项目~~
【分类号】：O626;R914;R96
，
本文编号：2468289
[Abstract]:In order to study the effect of unsaturated double bond modification in pyranone structure on the bioactivity of these compounds. Based on 5,6-dihydro-6-alkyl pyranone compounds, 5, 6 and 8 were designed and synthesized by modification of unsaturated double bonds. The inhibitory effects of the target compounds on human hepatoma cells (7721), human lung cancer cells (A549), human esophageal cancer cells (EC-109) and human gastric cancer cells (MGC-803) were evaluated by thiazole blue (MTT) assay. Compared with the positive drugs, it was found that except 4-(2,3,4,5-tetrafluoro) benzoyl amino-3-methyl-6-benzyloxy methyl-5,6-dihydro-pyran-2-one (6d), The inhibitory activity of the synthesized compounds on the proliferation of tumor cells disappeared. The results show that unsaturated double bonds play an important role in the structure of 5,6-dihydro-6-alkyl pyranones. It has the potential to improve its toxicity due to covalent bond binding.
【作者单位】： 郑州大学药学院;河北北方学院药学系;
【基金】：河南省高校科技创新人才计划(No.14HASTIT0031)资助项目~~
【分类号】：O626;R914;R96
，
本文编号：2468289
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