新型抗肿瘤药物 Ge132 衍生物的 DNA 结合特异性与细胞毒性
DNA binding specificity and cytotoxicity of novel antitumor agent Ge132 derivatives.
作者信息
Shangguan Guoqiang, Xing Feifei, Qu Xiaogang, Mao Jianhua, Zhao Dan, Zhao Xuejian, Ren Jinsong
机构信息
Division of Biological Inorganic Chemistry, Key Laboratory of Rare Earth Chemistry and Physics, Graduate School of the Chinese Academy of Sciences, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin 130022, China.
出版信息
Bioorg Med Chem Lett. 2005 Jun 15;15(12):2962-5. doi: 10.1016/j.bmcl.2005.04.053.
A series of Ge132 derivatives have shown enhanced antitumor activity. Previous studies suggest that DNA can be their primary target. Here we show direct evidence that two newly synthesized Ge132 derivatives can intercalate into DNA. Unexpected methyl substitution effect of the novel derivatives on DNA sequence selectivity and cytotoxicity was observed.
一系列锗-132衍生物已显示出增强的抗肿瘤活性。先前的研究表明DNA可能是它们的主要靶点。在此我们展示了直接证据，证明两种新合成的锗-132衍生物能够插入到DNA中。观察到了这些新型衍生物对DNA序列选择性和细胞毒性的意外甲基取代效应。
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