Selective Recognition of G-Quadruplex by Structural Tuning of Heteroaromatic Scaffolds and Side Chains

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2024 Mar 20

PMID 38505840

Authors

Khushnood Fatma

Prasanth Thumpati

Deepanjan Panda

Ravichandiran Velayutham

Jyotirmayee Dash

Affiliations

Soon will be listed here.

Abstract

In this study, carbazole () and dibenzofuran () derivatives were synthesized to examine their effect on the biomolecular recognition of G-quadruplex (G4) targets. Biophysical studies revealed that , a carbazole derivative, exhibits a specific affinity and effectively stabilizes the G4. Molecular modeling suggests a stable interaction of with the terminal G-tetrad of G4. Biological studies demonstrate that efficiently enters cells, reduces gene expression, and induces cell cycle arrest, DNA damage, and apoptosis in cancer cells. These findings demonstrate as a selective G4 ligand with therapeutic potential, providing insight into the structural basis of its anticancer mechanisms.

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