| 新型二氢化茚-咪唑衍生物的合成及生物活性研究 |
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| 引用本文： | 陈兴,夏沙,王少杰,陈文,周备,杨丽娟. 新型二氢化茚-咪唑衍生物的合成及生物活性研究[J]. 云南大学学报(自然科学版), 2015, 37(3): 422-428. DOI: 10.7540/j.ynu.20140686 |
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| 作者姓名： | 陈兴 夏沙 王少杰 陈文 周备 杨丽娟 |
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| 作者单位： | 1.云南民族大学 民族药资源化学国家民委-教育部重点实验室,云南 昆明 650500; |
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| 摘 要： | 从1-茚酮出发,通过简洁的路线合成了15个结构新颖的二氢化茚-咪唑衍生物,并对合成的新化合物进行了抗肿瘤活性和抑菌活性的筛选.生物活性结果表明,化合物7、15、16和18具有较好的抗肿瘤细胞毒活性,其中化合物15对白血病(HL-60)、肝癌(SMMC-7721)及肺癌(A-549)的细胞毒活性甚至优于阳性药物DDP;化合物7、10、14、15、16和17对金黄色葡萄球菌(S.aureus)和枯草芽孢杆菌(B.sutbilis)均具有较好的抑菌活性,化合物8对金黄色葡萄球菌显示出较好的选择性抑制活性.
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| 关 键 词： | 二氢化茚 咪唑 衍生物 抗肿瘤活性 抑菌活性 |
| 收稿时间： | 2014-12-19 |
Synthesis and biological activities of novel indane-imidazole derivatives |
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| CHEN Xing,XIA Sha,WANG Shao-jie,CHEN Wen,ZHOU Bei,YANG Li-juan. Synthesis and biological activities of novel indane-imidazole derivatives[J]. Journal of Yunnan University(Natural Sciences), 2015, 37(3): 422-428. DOI: 10.7540/j.ynu.20140686 |
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| Authors: | CHEN Xing XIA Sha WANG Shao-jie CHEN Wen ZHOU Bei YANG Li-juan |
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| Affiliation: | 1.Key Laboratory of Ethnic Medicine Resource Chemistry,State Ethnic Affairs Commission & Ministry of Education, Yunnan University of Nationalities,Kunming 650500,China; |
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| Abstract: | Fifteen novel indane-imidazole derivatives were prepared and evaluated in vitro against a panel of human tumor cell lines and bacterial activities.The results showed that the compounds 7,15,16 and 18 were found to have the most potent antitumor activities.In particular,compound 15 was found to be the most potent derivative and exhibited cytotoxic activity selectively against HL-60,SMMC-7721 and A-549 cell lines more sensitive to DDP.Compounds 7,10,14,15,16 and 17 have better antibacterial activity against S.aureus and B.subtilis,as well as compound 8 displayed selectively against S.aureus. |
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| Keywords: | indene imidazole derivatives antitumor activity antibacterial activity |
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