| 新型甾体N,N-二甲基缩氨硫腙类化合物的合成及其抗肿瘤活性 |
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| 引用本文： | 黄燕敏,郑嘉桦,赵丹丹,戚斌斌,杨春晖,盛海兵,甘春芳,崔建国.新型甾体N,N-二甲基缩氨硫腙类化合物的合成及其抗肿瘤活性[J].合成化学,2015,23(12):1106-1110. |
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| 作者姓名： | 黄燕敏 郑嘉桦 赵丹丹 戚斌斌 杨春晖 盛海兵 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，广西 南宁 530001 |
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| 基金项目： | 国家自然科学基金资助项目(21462009)； 南宁市科技开发项目（20145203） |
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| 摘 要： | 以乙醇（或甲醇为溶剂），冰醋酸为催化剂，去氢表雄酮、孕烯醇酮、雌酮和3,5-二羟基-6-甲酰基-B-降胆甾烷分别与N,N-二甲基硫代氨基脲经缩合反应，合成了4个新型的具有不同甾核结构特征的甾体N,N-二甲基缩氨硫腙类化合物（1～4），其结构经1H NMR， 13C NMR, IR和HR-EI-MS表征。采用MTT法测定了1~4对肝癌细胞(HepG)、人鼻咽癌细胞(CNE-2)和人肾上皮细胞（HEK-293T）的体外抑制细胞生长增殖活性。结果表明：1~3对HepG和CNE-2具有明显的抑制活性。
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| 关 键 词： | 甾酮 3 5-二羟基-6-甲酰基-B-降胆甾烷 N N-二甲基甾体缩氨硫腙 合成 抗肿瘤活性 |
| 收稿时间： | 2015-09-09 |
Synthesis and Anti-tumor Activities of Novel Steroidal N,N-dimethylthiosemicarbazone Compounds |
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| HUANG Yan-min,ZHENG Jia-hua,ZHAO Dan-dan,QI Bin-bin,YANG Chun hui,SHENG Hai-bing,GAN Chun-fang,CUI Jian-guo.Synthesis and Anti-tumor Activities of Novel Steroidal N,N-dimethylthiosemicarbazone Compounds[J].Chinese Journal of Synthetic Chemistry,2015,23(12):1106-1110. |
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| Authors: | HUANG Yan-min ZHENG Jia-hua ZHAO Dan-dan QI Bin-bin YANG Chun hui SHENG Hai-bing GAN Chun-fang CUI Jian-guo |
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| Institution: | College of Chemistry and Materials Science, Guangxi Teachers Education University, Nanning 53001, China |
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| Abstract: | Four novel N,N-dimethylthiosemicarbazone compounds(1~4) were synthesized by condensation reaction of dehydroepiandrosterone， pregnenolone, estrone, 3,5-dihydroxy-6-formyl-B-norcholestane with N,N-dimethylthiosemicarbazide, respectively, using EtOH(or MeOH) as solvent and HAc as catalyst. The structures were characterized by 1H NMR， 13C NMR, IR and HR-EI-MS. The anti-tumor activities of 1~4 against human hepatoma cells(HepG), nasopharyngeal carcinoma cells(CNE-2) and normal kidney epithelial cells(HEK293T) were investigated by MTT method. The results showed that 1~3 had better antiproliferative activities against HepG and CNE-2. |
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| Keywords: | sterone 3 5-dihydroxy-6-formyl-B-norcholestane steroidal N N-dimethylthiosemicarbazon synthesis anti-tumor activity |
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