Scherz Leon F, Abdel-Rahman Engy A, Ali Sameh S, Schlüter A Dieter, Abdel-Rahman Mona A
Institute of Polymers , Department of Materials , ETH Zürich , 8093 Zürich , Switzerland.
Pharmacology Department , Faculty of Medicine , Assiut University , 71515 Assiut , Egypt.
Medchemcomm. 2017 Feb 16;8(3):662-672. doi: 10.1039/c6md00728g. eCollection 2017 Mar 1.
A series of novel quinones was synthesized by reacting tetrabromo--benzoquinone with amino oligo(ethylene glycol) dendrons of generation numbers = 0-2. According to the performed shake-flask experiments, their aqueous solubility ( = 18 mg l-1.6 g ml) and partition coefficients (log = 2.53-0.21) can be tuned in a wide range as a function of . cytotoxicity assays of tetrabromo--benzoquinone and its derivatives against MCF-7 human breast cancer cells showed a concentration- and generation-specific biological activity with IC-values as low as 0.8 μM. Further investigations revealed a considerable selectivity against cancer cells, as indicated by a weak cytotoxicity against human skin fibroblast cells (>80% survival) within the studied range of concentrations. The results demonstrate that these novel amino oligo(ethylene glycol) dendrons depict versatile tools to ameliorate physical and pharmacological characteristics of extremely hydrophobic molecules and make them susceptible to biological applications.
通过使四溴 - 对苯醌与代数为0 - 2的氨基低聚（乙二醇）树枝状分子反应，合成了一系列新型醌类化合物。根据进行的摇瓶实验，它们的水溶性（ = 18 mg l - 1.6 g ml）和分配系数（log = 2.53 - 0.21）可以根据 在很宽的范围内进行调节。四溴 - 对苯醌及其衍生物对MCF - 7人乳腺癌细胞的细胞毒性测定显示出浓度和代数特异性的生物活性，IC值低至0.8 μM。进一步的研究表明，在所研究的浓度范围内，对人皮肤成纤维细胞的细胞毒性较弱（存活率> 80％），表明对癌细胞具有相当的选择性。结果表明，这些新型氨基低聚（乙二醇）树枝状分子是改善极疏水分子的物理和药理特性并使其易于生物应用的通用工具。
