| 雌酮芳杂环腙化合物的合成及抗肿瘤活性评估 |
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| 引用本文： | 赵丹丹,戚斌斌,杨雷,黄燕敏,甘春芳,崔建国.雌酮芳杂环腙化合物的合成及抗肿瘤活性评估[J].中国药物化学杂志,2014(6):470-474. |
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| 作者姓名： | 赵丹丹 戚斌斌 杨雷 黄燕敏 甘春芳 崔建国 |
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| 作者单位： | 广西师范学院化学与材料科学学院 |
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| 基金项目： | 广西省自然科学基金项目(2012GXNSFAA053018);广西省教育厅科研基金项目(200103YB067) |
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| 摘 要： | 目的设计合成某些雌酮芳杂环腙类化合物,并进行体外抗肿瘤活性测试。方法以雌酮为原料,通过雌酮与水合肼反应,生成雌酮-17-肼,然后该化合物与不同的芳香醛反应,得到雌酮芳杂环腙类化合物,并采用MTT法对目标化合物进行体外抑制肿瘤细胞增殖活性实验。结果与结论设计合成了5个雌酮芳杂环腙类化合物,活性研究表明,化合物7对宫颈癌细胞He La选择性地表现出较好的抑制增殖活性,IC50值为12.1μmol·L-1(顺铂的IC50值为10.1μmol·L-1)。
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| 关 键 词： | 雌酮 雌酮芳杂环腙 抗肿瘤活性 甾体芳杂环化合物 |
Synthesis of estrone aromatic heterocycle hydrazones and evaluation of their antiproliferative acitivity |
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| ZHAO Dan-dan;QI Bin-bin;YANG Lei;HUANG Yan-min;GAN Chun-fang;CUI Jian-guo.Synthesis of estrone aromatic heterocycle hydrazones and evaluation of their antiproliferative acitivity[J].Chinese Journal of Medicinal Chemistry,2014(6):470-474. |
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| Authors: | ZHAO Dan-dan;QI Bin-bin;YANG Lei;HUANG Yan-min;GAN Chun-fang;CUI Jian-guo |
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| Institution: | ZHAO Dan-dan;QI Bin-bin;YANG Lei;HUANG Yan-min;GAN Chun-fang;CUI Jian-guo;College of Chemistry and Material Engineering,Guangxi Teachers Education University; |
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| Abstract: | The estrone（ 1） is w idely applied in the cure of gynecological disease because of its special bioactivity. Using estrone as starting material,estrone-17-hydrazone（ 2） w as obtained by the reaction w ith hydrazine hydrate. Furthermore,the reaction of compound 2 w ith various aromatic aldehydes gave some estrone aromatic heterocycle hydrazones（ 3- 7）. The structures of all compounds w ere characterized by IR,NM R and M S. The antiproliferative activity of the compounds w as evaluated against human gastric cancer（ SGC-7901）,human liver cancer（ Bel-7404） and human cervical carcinoma（ He La） cells. The results show ed that compound 7 exhibited a significant inhibitory activity to He La cells w ith IC50 value of 12. 1 μmol·L^- 1（ cisplatin,IC50： 10. 1 μmol·L^- 1）. |
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| Keywords: | estrone estrone aromatic heterocycle hydrazones antiproliferative activity steroidal aromatic heterocyclic compound |
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