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荧光稠合咪唑并[4,5-]异喹啉与 GBB-3CR/亚氨酰化序列在 pUC-19 凝胶电泳迁移率变动分析中的 DNA 相互作用。

Fluorescent annulated imidazo[4,5-]isoquinolines a GBB-3CR/imidoylation sequence - DNA-interactions in pUC-19 gel electrophoresis mobility shift assay.

机构信息

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.

出版信息

Org Biomol Chem. 2022 May 4;20(17):3598-3604. doi: 10.1039/d2ob00372d.

Abstract

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.

摘要

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。

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