Institute of Organic Chemistry, Karlsruhe Institute of Technology (KIT), Fritz-Haber-Weg 6, 76131 Karlsruhe, Germany.
Institute of Applied Biosciences, Department of Food Chemistry and Toxicology, Karlsruhe Institute of Technology (KIT), Adenauerring 20, 76131 Karlsruhe, Germany.
Org Biomol Chem. 2022 May 4;20(17):3598-3604. doi: 10.1039/d2ob00372d.
Herein we report the development of a sequential synthesis route towards annulated imidazo[4,5-]isoquinolines comprising a GBB-3CR, followed by an intramolecular imidoylative cyclisation. X-Ray crystallography revealed a flat 3D structure of the obtained polyheterocycles. Thus, we evaluated their interactions with double-stranded DNA by establishing a pUC-19 plasmid-based gel electrophoresis mobility shift assay, revealing a stabilising effect on ds-DNA against strand-break inducing conditions.
在此,我们报告了一种环化咪唑并[4,5-]异喹啉的连续合成途径的发展,该途径包括 GBB-3CR,随后是分子内酰亚胺环化。X 射线晶体学揭示了所得到的多杂环的平面 3D 结构。因此,我们通过建立基于 pUC-19 质粒的凝胶电泳迁移率变动分析评估了它们与双链 DNA 的相互作用,揭示了它们对双链 DNA 的稳定作用,可抵抗诱导链断裂的条件。