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Macrocyclic G-Quadruplex Ligands

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G-quadruplex stabilizing compounds have recently received increased interest due to their potential application as anticancer therapeutics. A significant number of structurally diverse G-quadruplex ligands have been developed. Some of the most potent and selective ligands currently known are macrocyclic structures which have been modeled after the natural product telomestatin or from porphyrin-based ligands discovered in the late 1990s. These two structural classes of G-quadruplex ligands are reviewed here with special attention to selectivity and structure-activity relationships, and with focus on the recent developments.

Keywords: Anticancer therapeutics; BCL-2; Corroles; DNA; FRET Tm; G-quadruplex; HeLa cells; Hoogsteen base pairing; SPR; Streptomyces anulatus; Telomeres; WO 0024747; WO 2004078764; antitumor; c-KIT sequence; c-MYC; cancer; cell line; cytotoxic; drug discovery; guanine; hexaoxazoles; hybrid; isoindole; leukemia; ligands; macrocycles; macrocyclic; nucleic acid; oncogenes; p-p stacking; phosphate backbone; porphyrin; porphyrins; pyrrole; telomerase-negative Saos-2 cells; telomere repeat amplification protocol (TRAP) assay; telomeric sequences; telomestatin; topology; tumor xenografts

Document Type: Research Article


Publication date: October 1, 2010

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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