| 3-芳基苯并呋喃酮类化合物的合成及抗肿瘤活性 |
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| 引用本文： | 吕泽良,高扬,李军,黄桐堃,何树杰,邹永.3-芳基苯并呋喃酮类化合物的合成及抗肿瘤活性[J].高等学校化学学报,2013,34(11):2531. |
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| 作者姓名： | 吕泽良 高扬 李军 黄桐堃 何树杰 邹永 |
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| 作者单位： | 1. 中国科学院广州化学研究所, 广州 510650;
2. 中国科学院大学, 北京 100049;
3. 曲靖师范学院化学化工学院, 曲靖 655011;
4. 浙江大学医学院附属第二医院, 杭州 313000 |
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| 基金项目： | 国家自然科学基金(批准号:21272280)、广东省中国科学院全面战略合作项目(批准号:2009B091300125)、广东省战略新兴产业核心技术攻关项目(批准号:2011A081401002)、"十二五"国家重大新药创制项目(批准号:2011ZX09202-101-07)和广州市科技计划项目(批准号:2012J4300097)资助. |
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| 摘 要： | 以甲氧基取代苯甲醛和氯仿为起始物, 以四丁基溴化铵(TBAB)为催化剂, 在氢氧化钠溶液中反应制得甲氧基取代扁桃酸钠, 经酸化得到相应的甲氧基取代扁桃酸; 在三氟化硼-乙醚催化下, 甲氧基取代扁桃酸分别与不同的酚类化合物发生串联的酯化-分子内环合反应, 便捷、 高效地合成了13种3-芳基苯并呋喃酮类化合物. 采用噻唑蓝(MTT)法对其中11种化合物进行了肿瘤细胞增殖抑制活性研究, 结果表明化合物4a, 4j及4a, 4i具有较强的抗肿瘤活性.
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| 关 键 词： | 3-芳基苯并呋喃酮 甲氧基取代扁桃酸 酚类 抗肿瘤活性 |
| 收稿时间： | 2013-03-01 |
Synthesis and Antitumor Activities of 3-Arylbenzofunanone Analogues |
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| LV Ze-Liang,GAO Yang,LI Jun,HUANG Tong-Kun,HE Shu-Jie,ZOU Yong.Synthesis and Antitumor Activities of 3-Arylbenzofunanone Analogues[J].Chemical Research In Chinese Universities,2013,34(11):2531. |
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| Authors: | LV Ze-Liang GAO Yang LI Jun HUANG Tong-Kun HE Shu-Jie ZOU Yong |
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| Institution: | 1. Guangzhou Institute of Chemistry, Chinese Academy of Sciences, Guangzhou 510650, China;
2. University of Chinese Academy of Sciences, Beijing 100049, China;
3. College of Chemistry and Chemical Engineering, Qujing Normal University, Qujing 655011, China;
4. The Second Afflilated Hospital, School of Medicine, Zhejiang University, Hangzhou 313000, China |
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| Abstract: | Starting from methoxyl-substituted benzaldehydes and chloroform, a series of methoxyl-substituted mandelic sodium salts were synthesized in the presence of sodium hydroxide and catalytic amount of tetrabuty-lammonium bromide(TBAB), the corresponding methoxyl-substituted mandelic acids could readily be obtained by acidification. These intermediates on reaction with various substituted phenols in the presence of boron trifluoride etherate via a sequential esterification-alkylation process to give 13 3-arylbenzofunanone analogues in high yields with simple procedures. The inhibitory effects of 11 compounds on cell proliferation were investigated by methylthiazolyldiphenyl-tetrazolium bromide(MTT) method using SW620, A549 and MNNG/HOS cell lines. The results showed that the 3-arylbenzofunanone analogues 4a, 4j and 4a, 4i exhibited some activities against the proliferation of the cell lines. |
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| Keywords: | 3-Arylbenzofunanone Methoxyl-substituted mandelic acid Phenol Antitumor activity |
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