Department of Organic Chemistry, Institute of Chemistry, Faculty of Science, P.J.Šafárik University, Moyzesova 11, Košice, Slovak Republic.
Department of Biochemistry, Institute of Chemistry, Faculty of Science, P.J.Šafárik University, Moyzesova 11, Košice, Slovak Republic.
Spectrochim Acta A Mol Biomol Spectrosc. 2017 Jun 5;180:234-241. doi: 10.1016/j.saa.2017.03.014. Epub 2017 Mar 8.
This paper describes the synthesis of a novel series of acridine thiosemicarbazones through a two-step reaction between various isothiocyanates and hydrazine followed by treatment with acridin-9-carbaldehyde. The properties of this series of seven new derivatives are studied using NMR and biochemical techniques, and the DNA-binding properties of the compounds are determined using spectrophotometric studies (UV-vis absorption, fluorescence, and circular/linear dichroism) and viscometry. The binding constants K are estimated as being in the range of 2.2 to 7.8×10M and the percentage of hypochromism was found to be 22.11-49.75% (from UV-vis spectral titration). Electrophoretic experiments prove that the novel compounds demonstrate moderate inhibitory effects against Topo I activity at a concentration of 60×10M.
本文通过各种异硫氰酸酯与水合肼的两步反应以及与吖啶-9-甲醛的后续处理，合成了一系列新型吖啶硫代缩氨基脲。采用 NMR 和生化技术研究了这一系列七个新衍生物的性质，并通过分光光度研究（紫外可见吸收、荧光和圆/线二色性）和粘度法确定了化合物的 DNA 结合性质。结合常数 K 的估计范围为 2.2 到 7.8×10M，并且从紫外可见光谱滴定中发现消光率为 22.11-49.75%。电泳实验证明，在 60×10M 的浓度下，这些新型化合物对拓扑异构酶 I 活性表现出中等抑制作用。
