Department of Organic Chemistry, Medical University, Białystok, Poland.
J Enzyme Inhib Med Chem. 2010 Oct;25(5):629-34. doi: 10.3109/14756360903389872.
The biological evaluation of carbocyclic minor groove binders 1-6 is described. The cytotoxicity of the obtained compounds was tested on MDA-MB-231 breast cancer cells. The mechanism of action of compounds 1-6 was studied employing the topoisomerase I/II inhibition assay and ethidium displacement assay using pBR322. Determination of association constants was done using calf thymus DNA, T4 coliphage DNA, poly(dA-dT)(2), and poly(dG-dC)(2). The effect of compounds 1-6 on the amidolytic activity of plasmin, trypsin, thrombin, and urokinase was also examined.
本文描述了碳环类小分子沟结合物 1-6 的生物学评价。对所得化合物的细胞毒性进行了 MDA-MB-231 乳腺癌细胞试验。采用拓扑异构酶 I/II 抑制试验和 pBR322 的溴化乙锭置换试验研究了化合物 1-6 的作用机制。使用小牛胸腺 DNA、T4 噬菌体 DNA、聚（dA-dT）（2）和聚（dG-dC）（2）测定了结合常数。还研究了化合物 1-6 对纤溶酶、胰蛋白酶、凝血酶和尿激酶的 amidolytic 活性的影响。
