Journal
CHEMICAL COMMUNICATIONS
Volume 47, Issue 2, Pages 719-721Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c0cc03641b
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Funding
- Area of Excellence Scheme [AoE/P-10/01]
- Innovation and Technology Fund [ITF-Tier 2, ITS/134/09FP]
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A platinum(II)-based major groove binder [Pt-II(C boolean AND N) (C NR)(2)](+) (HC boolean AND N = 2-phenylpyridine (phpy), R = 2-naphthyl) was identified as a potent human topoisomerase II alpha poison. It stabilizes the covalent TopoII alpha-DNA cleavage complex and induces cancer cell death with potency significantly higher than the widely clinically used TopoII alpha poison Vp-16.
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