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首页> 外文期刊>Anticancer Research: International Journal of Cancer Research and Treatment >Further Quantitative Structure-Cytotoxicity Relationship Analysis of 3-Styrylchromones
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Further Quantitative Structure-Cytotoxicity Relationship Analysis of 3-Styrylchromones

机译：3- styrylchroomones的进一步定量结构 - 细胞毒性关系分析

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Background/Aim: Very few studies are available about the biological activity of 3-styrylchromones. Our previous study demonstrated the importance of methoxy group at 6-position of the chromone ring and hydroxyl group at 4'-position of phenyl group in styryl moiety. As a sequel of this study, we synthesized fourteen compounds that include eight 3-styrylchromones where methoxy group was introduced at 7-position of chromone rings, and then evaluated their tumor-specificity. Materials and Methods: Tumor-specificity (TS) was calculated by relative cytotoxicity against human oral squamous cell carcinoma cell lines versus human normal oral cells. Apoptosis induction and growth arrest were monitored by cell-cycle analysis. Quantitative structure-activity relationship analysis of TS was performed with 3,167 chemical descriptors. Results and Discussion: Two compounds, 7methoxy-3-[(1E)-2-phenylethenyl]-4H-1-benzopyran-4-one [7] and 3-[(1E)-2-(4-hydroxyphenyl)ethenyl]-7-methoxy-4H-1benzopyran-4-one [14] showed higher tumor-specificity than doxorubicin and 5-FU, suggesting the importance of methoxy group in 7-position of the chromone ring. These compounds induced the apoptosis and mitotic arrest in HSC-2 cells. The tumor-specificity of 3-styrylchromone derivatives were most correlated with descriptors for molecule shape and electronic charge. The present study suggested that modification by introducing methoxy group at 7-position, instead at 6-position, further increased the tumor-specificity of 3-styrylchromone.
机译：背景/目的：少数研究有关3-苯乙烯铬酮的生物活性。我们以前的研究证明甲氧基在铬基环和羟基的6-位在苯基中的苯基中的6-位置的重要性。作为本研究的续集，我们合成了十四种化合物，包括八个3-苯乙烯酮，其中甲氧基在铬酮环的7-位引入，然后评估其肿瘤特异性。材料和方法：肿瘤特异性（TS）通过对人口腔鳞状细胞癌细胞系的相对细胞毒性计算，与人正常口腔细胞。通过细胞循环分析监测凋亡诱导和生长停滞。用3,167化学描述符进行TS的定量结构 - 活性关系分析。结果与讨论：两种化合物，7甲氧基-3 - [（1E）-2-苯基乙烯基] -4H-1-苯并吡喃-4-一[7]和3 - [（1E）-2-（4-羟基苯基）乙烯基] -7-甲氧基-4H-1Bendopyran-4-one [14]显示出比多柔比星和5-FU更高的肿瘤特异性，表明甲氧基在铬酮环的7位的重要性。这些化合物在HSC-2细胞中诱导细胞凋亡和有丝分裂。 3-苯乙烯铬酮衍生物的肿瘤特异性与分子形状和电子电荷的描述符最相关。本研究表明，通过在7-位引入甲氧基，而不是在6位，进一步增加了3-苯乙烯克罗姆松的肿瘤特异性来修饰。

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