Understanding the Binding Mechanism of a Pyrazino[1,2‐a]indole Derivative with Calf Thymus DNA

Abstract

This work was focused on understanding the interaction mechanism of pyrazino[1,2‐a]indole derivative in calf thymus DNA (ctDNA) using various spectroscopy and computational techniques. The UV‐Vis absorption result shows that the binding interaction of pyrazino[1,2‐a]indole derivative in ctDNA complex may be in the non –covalent form and the binding associate constant Ka value was estimated 7.06×103 L mol−1 at 297 K. The fluorescence emission spectroscopy analysis suggested that pyrazino[1,2‐a]indole derivative quenching mechanism in ctDNA mainly due to the static nature and thermodynamical parameter analysis implied the binding of pyrazino[1,2‐a]indole derivative in ctDNA mainly due to hydrophobic force. Forster resonance energy transfer analysis was also calculated and the r=2.1 nm. Circular dichroism spectra conclude that there is a change in the secondary structural region of ctDNA due to an interaction with pyrazino[1,2‐a]indole derivative. Together with the molecular docking studies, hydrophobic nature of the interaction of pyrazino[1,2‐a]indole derivative with ctDNA might be deduced.

Time‐resolved emission spectroscopy to elucidate the functional nature of heat‐stable transcription factor

“…From the plot, the binding constant K a = 4.75 × 10 6 L mol −1 is calculated and the number of binding sites for ctDNA n = 1.03. From the result, it is clear that the protein binds to DNA 17 . It can also be observed that the binding is class one that is, the protein has one possible site for the ctDNA to bind.…”

“…From the result, it is clear that the protein binds to DNA. 17 It can also be observed that the binding is class one that is, the protein has one possible site for the ctDNA to bind.…”

Chemoselective Divergent Transformations of N-(Propargyl)indole-2-carbonitriles with Nitrogen Nucleophiles: Alkyne Hydroamination or Domino Cyclizations

“…3 The synthesis of annulated indoles attracts much attention too, e.g., pyrazino[1,2-a]indoles 4 are sought for heterocycles with a diverse array of biological activities. 5 Some representative examples, most relevant to current research, display antiproliferative activity, 6 bind to DNA, 7 and inhibit CK2, PIM1, and PIM2 8,9 (Figure 1).…”