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A Cyclometallated Iridium(III) Complex As a c-myc G-Quadruplex Stabilizer and Down-Regulator of c-myc Oncogene Expression

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Abstract:

A new cyclometallated iridium(III) complex with the 2,2'-biquinoline N-donor ligand has been synthesized and characterized. The interaction and affinity of the complex towards c-myc G-quadruplex and duplex DNA have been investigated using UV/Vis spectroscopy and gel mobility shift assay. These studies revealed that complex 1 binds to c-myc G-quadruplexes (Pu22 and Pu27) with high affinity but does not interact with duplex DNA either by intercalation or groove binding. The ability of 1 to stabilize c-myc G-quadruplex DNA in vitro has also been examined through a PCR stop assay and a cell-based luciferase reporter assay. Complex 1 displays promising cytotoxic activity against the HeLa cell line with sub-micromolar potency.

Keywords: 2; 2'-biquinoline N-donor; DNA; G-quadruplex; c-myc; cyclometallated iridium(III) complex; iridium(III); metal complex; oncogene; promoter

Document Type: Research Article

DOI: https://doi.org/10.2174/092986713804910175

Publication date: 2013-02-01

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