Biological and Medicinal Chemistry

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

Authors

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.

Content

Thumbnail image of Core Diversification Manuscript v0.8.pdf

Supplementary material

Thumbnail image of Core Diversification SI v0.8.pdf
Core Diversification SI v0.8