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。
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 that the synthetics H6 and H99 have marked anti-tumor effects in vitro.
出处
《解放军药学学报》
CAS
2009年第6期482-485,共4页
Pharmaceutical Journal of Chinese People's Liberation Army
基金
国家自然科学基金资助项目
No.30772628
关键词
组蛋白去乙酰化酶
抗瘤活性
体外
histone deacetylases anti-tumor activity in vitro
