Department of Chemistry, Faculty of Science, Gazi University, Teknikokullar, Ankara 06500, Turkey; University of Siegen, Organic Chemistry II, Adolf-Reichwein-Str. 2, D-57068 Siegen, Germany.
University of Siegen, Organic Chemistry II, Adolf-Reichwein-Str. 2, D-57068 Siegen, Germany.
Spectrochim Acta A Mol Biomol Spectrosc. 2018 May 5;196:432-438. doi: 10.1016/j.saa.2018.02.051. Epub 2018 Feb 20.
An improved microwave-induced synthesis of five ethidium derivatives (Ethidium derivatives, 2a-d) is presented. As the derivatives 2a-d have been proposed previously to be telomerase inhibitors, the binding interactions of these ethidium derivatives with G-quadruplex DNA were evaluated by means of photometric and fluorimetric titration, thermal DNA denaturation, CD and H NMR spectroscopy. In particular, the compound bearing 3,8-bis(pyrrolidin-1-yl)propanamido substituent 2a exhibits high selectivity for G-quadruplex DNA relative to duplex DNA.
介绍了一种改进的微波诱导合成五种吖啶衍生物（吖啶衍生物 2a-d）的方法。由于这些衍生物 2a-d 先前被提议为端粒酶抑制剂，因此通过光度和荧光滴定、热 DNA 变性、CD 和 H NMR 光谱法评估了这些吖啶衍生物与 G-四链体 DNA 的结合相互作用。特别是，带有 3,8-双（吡咯烷-1-基）丙酰胺取代基的化合物 2a 相对于双链 DNA 对 G-四链体 DNA 表现出高选择性。
