Ravera, Mauro, Gabano, Elisabetta, Zanellato, Ilaria, Fregonese, Federico, Pelosi, Giorgio, Platts, James Alexis ![]() |
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Abstract
We report studies of a novel series of Pt(IV) complexes exhibiting an asymmetric combination of acetylamido and carboxylato ligands in the axial positions. We demonstrate efficient synthesis of a series of analogues, differing in alkyl chain length and hence lipophilicity, from a stable acetylamido/hydroxido complex formed by reaction of cisplatin with peroxyacetimidic acid (PAIA). NMR spectroscopy and X-ray crystallography confirm the identity of the resulting complexes, and highlight subtle differences in structure and stability of acetylamido complexes compared to equivalent acetato complexes. Reduction of acetylamido complexes, whether achieved chemically or electro-chemically, is significantly more difficult than of acetate complexes, resulting in lower antiproliferative activity for shorter-chain complexes. For those with longer chains and hence greater cell uptake, this difference is negated and acetylamido complexes are as active as acetato analogues, both exhibiting antiproliferative potency (1/IC50) against A2780 ovarian cancer cells similar to that of cisplatin.
Item Type: | Article |
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Date Type: | Published Online |
Status: | Published |
Schools: | Advanced Research Computing @ Cardiff (ARCCA) Chemistry |
Subjects: | Q Science > QD Chemistry |
Publisher: | Royal Society of Chemistry |
ISSN: | 1477-9226 |
Date of First Compliant Deposit: | 30 March 2016 |
Date of Acceptance: | 2 February 2016 |
Last Modified: | 07 Nov 2023 00:15 |
URI: | https://orca.cardiff.ac.uk/id/eprint/86539 |
Citation Data
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