Imide Condensation as a Strategy for the Synthesis of Core Diversified G-Quadruplex Ligands with Anti-Cancer and Anti-Parasitic Activity

13 March 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A facile imide coupling strategy for the one-step preparation of G‑quadruplex ligands with varied core chemistries is described. The G‑quadruplex stabilization, anticancer and antiparasitic activity of a library of nine compounds was examined, identifying a nanomolar inhibitor of T. brucei with 78‑fold selectivity over MRC5 cells, and strong stabilization of G‑quadruplex nucleic acids.

Keywords

G-quadruplexes
Ligand Design Approach
DNA
anticancer drugs
antiparasitic agent

Supplementary materials

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Core Diversification SI v0.8
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