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Issue 38, 2012
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Pt(II) squares as selective and effective human telomeric G-quadruplex binders and potential cancer therapeutics

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Abstract

A series of four self-assembled Pt(II) molecular squares with 4,4′-dipyridyl or pyrazine bridges, including the previously reported Pt(II) squares [Pt(en)(4,4′-dipyridyl)]4(NO3)8 (1), were investigated for their abilities to act as selective and effective human telomeric (htelo) G-quadruplex binders. FRET and SPR studies demonstrated that Pt(II) squares could discriminate against duplex DNA, and show promising selectivity between intramolecular G-quadruplexes. PCR-stop assays and CD studies showed that Pt(II) squares strongly induced the formation of parallel G-quadruplexes. ITC experiments indicated that Pt(II) squares could bind to the G-quadruplex with high binding constants (Kb values ranging from 104–108 M−1). All four Pt(II) squares were effective inhibitors of human telomerase, and showed anticancer efficacy. This was particularly the case for [Pt(NH3)2(4,4′-dipyridyl)]4(NO3)8 (2), which exhibited a 15-fold higher antiproliferative effect on A549/cisR cells than cisplatin.

Graphical abstract: Pt(ii) squares as selective and effective human telomeric G-quadruplex binders and potential cancer therapeutics

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Publication details

The article was received on 18 Jun 2012, accepted on 31 Jul 2012 and first published on 02 Aug 2012


Article type: Paper
DOI: 10.1039/C2DT31303K
Citation: Dalton Trans., 2012,41, 11807-11812
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    Pt(II) squares as selective and effective human telomeric G-quadruplex binders and potential cancer therapeutics

    X. Zheng, Y. Zhong, C. Tan, L. Ji and Z. Mao, Dalton Trans., 2012, 41, 11807
    DOI: 10.1039/C2DT31303K

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