Potent and Selective Cytotoxic and Anti-inflammatory Gold(III) Compounds Containing Cyclometalated Phosphine Sulfide Ligands.

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ID: 85616
2019
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Abstract
Four cycloaurated phosphine sulfide complexes, [Au{κ -2-C H P(S)Ph } ][AuX ] [X=Cl (2), Br (3), I (4)] and [Au{κ -2-C H P(S)Ph } ]PF (5), have been prepared and thoroughly characterized. The compounds were found to be stable under physiological-like conditions and showed excellent cytotoxicity against a broad range of cancer cell lines and remarkable cytotoxicity in 3D tumor spheroids. Mechanistic studies with cervical cancer (HeLa) cells indicated that the cytotoxic effects of the compounds involve the inhibition of thioredoxin reductase and induction of apoptosis through mitochondrial disruption. In vivo experiments in nude mice bearing HeLa xenografts showed that treatment with compounds 4 and 5 resulted in significant inhibition of tumor growth (35.8 and 46.9 %, respectively), better than that of cisplatin (29 %). The newly synthesized gold complexes were also evaluated for their in vitro and in vivo anti-inflammatory activity through the study of lipopolysaccharide (LPS)-activated macrophages and carrageenan-induced hind paw edema in rats, respectively.
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reddy2019potentchemistry Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Reddy, T Srinivasa;Pooja, Deep;Privér, Steven H;Luwor, Rodney B;Mirzadeh, Nedaossadat;Ramesan, Shwathy;Ramakrishna, Sistla;Karri, Shailaja;Kuncha, Madhusudana;Bhargava, Suresh K;
Journal Chemistry (Weinheim an der Bergstrasse, Germany)
Year 2019
DOI
10.1002/chem.201903388
URL
Keywords
Cytotoxicity gold antitumor agents anti-inflammatory agents phosphine sulfide ligands

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