【摘要】：為了研究吡喃酮結(jié)構(gòu)中不飽和雙鍵修飾對該類化合物生物活性的影響.基于5,6-二氫-6-烷基吡喃酮類化合物哥納香甲素,通過不飽和雙鍵的修飾,設(shè)計合成了化合物5,6和8.利用噻唑藍(lán)(MTT)法評價了目標(biāo)化合物對人肝癌細(xì)胞(7721)、人肺癌細(xì)胞(A549)、人食管癌細(xì)胞(EC-109)、人胃癌細(xì)胞(MGC-803)的細(xì)胞增殖抑制活性.通過和陽性藥物的對比發(fā)現(xiàn),除了4-(2,3,4,5-四氟)苯甲酰氨基-3-甲基-6-芐氧甲基-5,6-二氫-吡喃-2-酮(6d),所合成化合物的腫瘤細(xì)胞增殖抑制活性均消失.結(jié)果表明,在5,6-二氫-6-烷基吡喃酮類化合物結(jié)構(gòu)中,不飽和雙鍵起著至關(guān)重要的作用,對其進(jìn)行適當(dāng)?shù)男揎?在保留其活性的同時,具有潛在改善其因共價鍵結(jié)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.
【作者單位】： 鄭州大學(xué)藥學(xué)院;河北北方學(xué)院藥學(xué)系;
【基金】：河南省高�？萍紕�(chuàng)新人才計劃(No.14HASTIT0031)資助項目~~
【分類號】：O626;R914;R96
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本文編號：2468289