| 靶向组蛋白去乙酰化酶新型化合物的体外抗肿瘤活性筛选 |
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| 引用本文： | 王立杰,孙丽,韩春光,高志清,王琼,赵砚瑾,李庶心,刘永学.靶向组蛋白去乙酰化酶新型化合物的体外抗肿瘤活性筛选[J].解放军药学学报,2009,25(6):482-485. |
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| 作者姓名： | 王立杰 孙丽 韩春光 高志清 王琼 赵砚瑾 李庶心 刘永学 |
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| 作者单位： | 1. 军事医学科学院放射与辐射医学研究所,北京,100850
2. 军事医学科学院放射与辐射医学研究所,北京,100850;江西中医学院,江西,南昌,330004 |
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| 摘 要： | 目的针对组蛋白去乙酰化酶（HDAC）,自行设计合成系列化合物,着重对其体外抗肿瘤活性进行筛选,为进一步优化设计提供借鉴。方法首先利用MTT法测定各化合物对不同肿瘤细胞株增殖能力的影响,再对重点化合物进行组蛋白去乙酰化酶抑制活性测定。结果MTT结果显示,化合物H6和H99均显示出较好的肿瘤细胞增殖抑制效应;相应的HDAC活性检测表明,二者亦具有肯定的HDAC抑制效应。结论化合物H6和H99具有明显的体外抗瘤活性,值得深入研究。
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| 关 键 词： | 组蛋白去乙酰化酶 抗瘤活性 体外 |
Screening the in Vitro Anti-tumor Activities of Novel Synthetics Targeting to Histone Deacetylases1 |
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| WANG Li-Jie,SUN Li,HAN Chun-Guang,GAO Zhi-Qing,WANG Qiong,ZHAO Yan-Jin,LI Shu-Xin,LIU Yong-Xue.Screening the in Vitro Anti-tumor Activities of Novel Synthetics Targeting to Histone Deacetylases1[J].Pharmaceutical Journal of Chinese People's Liberation Army,2009,25(6):482-485. |
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| Authors: | WANG Li-Jie SUN Li HAN Chun-Guang GAO Zhi-Qing WANG Qiong ZHAO Yan-Jin LI Shu-Xin LIU Yong-Xue |
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| Institution: | (Beijing Institute of Radiation Medicine,Beijing 100850 China;Department of Pharmacology,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,Jiangxi China) |
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| Abstract: | Aim To evaluate the antitumor effects of the synthetics targeting to histone deacetylases (HDAC).Methods The anti-proliferative activities of the synthetics on various human tumor cells were screened using MTT assay in vitro.Then,some screened synthetics were detected for their inhibition on HDAC.Results The synthetics H6 and H99 exert their inhibitive effects on the proliferation of several human cancer cell lines.Also,they have the properties to inhibit the activities of HDAC.Conclusion It has been proven... |
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| Keywords: | histone deacetylases anti-tumor activity in vitro |
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