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

Author(s): H. Yang, V. P.-Y. Ma, D. S.-H. Chan, H.-Z. He, C.-H. Leung, D.-L. Ma

Journal Name: Current Medicinal Chemistry

Volume 20 , Issue 4 , 2013

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

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Article Details

Year: 2013
Published on: 17 January, 2013
Page: [576 - 582]
Pages: 7
DOI: 10.2174/0929867311320040009
Price: $65

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