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



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.


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Supplementary material

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Core Diversification SI v0.8