Synthesis and g-quadruplex-binding properties of defined acridine oligomers

特定吖啶寡聚体的合成及其与 g-四链体结合的特性

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作者:Rubén Ferreira, Anna Aviñó, Ricardo Pérez-Tomás, Raimundo Gargallo, Ramon Eritja

Abstract

The synthesis of oligomers containing two or three acridine units linked through 2-aminoethylglycine using solid-phase methodology is described. Subsequent studies on cell viability showed that these compounds are not cytotoxic. Binding to several DNA structures was studied by competitive dialysis, which showed a clear affinity for DNA sequences that form G-quadruplexes and parallel triplexes. The fluorescence spectra of acridine oligomers were affected strongly upon binding to DNA. These spectral changes were used to calculate the binding constants (K). Log K were found to be in the order of 4-6.

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