Yao, K;
Karunanithy, G;
Howarth, A;
Holdship, P;
Thompson, AL;
Christensen, KE;
Baldwin, AJ;
... Farrer, NJ; + view all
(2021)
Cell-permeable lanthanide-platinum(iv) anti-cancer prodrugs.
Dalton Transactions
10.1039/d1dt01688a.
(In press).
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Abstract
Platinum compounds are a vital part of our anti-cancer arsenal, and determining the location and speciation of platinum compounds is crucial. We have synthesised a lanthanide complex bearing a salicylic group (Ln = Gd, Eu) which demonstrates excellent cellular accumulation and minimal cytotoxicity. Derivatisation enabled access to bimetallic lanthanide–platinum(II) and lanthanide–platinum(IV) complexes. Luminescence from the europium–platinum(IV) system was quenched, and reduction to platinum(II) with ascorbic acid resulted in a “switch-on” luminescence enhancement. We used diffusion-based 1H NMR spectroscopic methods to quantify cellular accumulation. The gadolinium–platinum(II) and gadolinium–platinum(IV) complexes demonstrated appreciable cytotoxicity. A longer delay following incubation before cytotoxicity was observed for the gadolinium–platinum(IV) compared to the gadolinium–platinum(II) complex. Functionalisation with octanoate ligands resulted in enhanced cellular accumulation and an even greater latency in cytotoxicity.
| Type: | Article |
|---|---|
| Title: | Cell-permeable lanthanide-platinum(iv) anti-cancer prodrugs |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1039/d1dt01688a |
| Publisher version: | http://doi.org/10.1039/d1dt01688a |
| Language: | English |
| Additional information: | This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ |
| Keywords: | Science & Technology, Physical Sciences, Chemistry, Inorganic & Nuclear, Chemistry, NEAR-INFRARED EMISSION, LANTHANIDE COMPLEXES, CONTRAST AGENTS, OPTICAL PROBES, MODEL, NMR, CISPLATIN, DIFFUSION, BINDING, SYSTEMS |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Structural and Molecular Biology |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10129599 |
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