{
  "abstract": "Imidazole- and benzimidazole-based Au­(I) N-heterocyclic carbene (NHC) complexes show great potency as anticancer agents. However, other NHC scaffolds are only sparsely explored. Four gold­(I) NHC complexes featuring thiazolium-based ligands (NHCthia) with varying N-substituents were synthesized and evaluated for their biological activity. The complexes containing aromatic N-substituents demonstrate higher stability, higher TrxR inhibition, and activity against breast (MDA-MB-231 and MCF-7) and ovarian (A2780) cancer cell lines, compared to the tested alkyl N-substituted complexes. Specifically, mesityl-substituted complex 1 exhibits high activity with IC50 values in the nanomolar range, exceeding the potency of auranofin in MDA-MB-231 cells. Mechanistic studies in leukemia cells (Nalm-6) revealed that complex 1 induces ROS formation, activates BAX and BAK, and causes mitochondrial membrane potential loss, initiating intrinsic apoptosis. Notably, the ligand precursor L1 shows no significant cytotoxicity, confirming that the gold­(I) moiety drives the activity. Additionally, complex 1 can overcome resistance to etoposide and prednisolone without affecting healthy leukocytes, making Au­(I) bis-NHCthia complexes a compelling class of antiproliferative agents.",
  "abstract_shown": true,
  "affiliations": [
    "TUM School of Natural Science, Department of Chemistry and Catalysis Research Centre, Molecular Catalysis, Technical University of Munich, Lichtenbergstr. 4, 85748 Garching bei München, Germany",
    "Department of Human Medicine, MSH Medical School Hamburg, am Kaiserkai 1, 20457 Hamburg, Germany",
    "Centro de Ciências e Tecnologias Nucleares and Departamento de Engenharia e Ciências Nucleares, Instituto Superior Técnico, CTN, Universidade de Lisboa, Estrada Nacional 10 (km 139,7), 2695-066 Bobadela LRS, Portugal",
    "Department of Pediatric Hematology/Oncology, HELIOS Clinics Schwerin, Wismarsche Strasse 393-397, 19055 Schwerin, Germany",
    "Universität Potsdam, Karl-Liebknecht-Str. 24-25, 14476 Potsdam, Germany"
  ],
  "article_type": "research article",
  "arxiv": null,
  "author_total": 9,
  "authors": [
    {
      "affs": [
        0
      ],
      "name": "Melanie E. Hoffmann"
    },
    {
      "affs": [
        1
      ],
      "name": "Lisa C. Haas"
    },
    {
      "affs": [
        2
      ],
      "name": "Fernanda Marques"
    },
    {
      "affs": [
        1
      ],
      "name": "Sarah Sarwary"
    },
    {
      "affs": [
        3,
        4
      ],
      "name": "Charlotte Theile"
    },
    {
      "affs": [
        1,
        3
      ],
      "name": "Bakr Mustafa"
    },
    {
      "affs": [
        2
      ],
      "name": "João D. G. Correia",
      "orcid": "0000-0002-7847-4906"
    },
    {
      "affs": [
        1,
        3
      ],
      "name": "Aram Prokop"
    },
    {
      "affs": [
        0
      ],
      "name": "Fritz E. Kühn",
      "orcid": "0000-0002-4156-780X"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/a63zk9fbn7bz7.bib",
  "cited_by": 0,
  "doi": "10.1021/acs.inorgchem.6c02992",
  "fulltext_url": "https://pmc.ncbi.nlm.nih.gov/articles/PMC13715578/",
  "id": "a63zk9fbn7bz7",
  "issns": [
    "0020-1669",
    "1520-510X"
  ],
  "landing_url": "https://doi.org/10.1021/acs.inorgchem.6c02992",
  "language": "en",
  "licence": "CC-BY-4.0",
  "licence_label": "CC BY 4.0",
  "licence_source": "article",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "heading",
      "Article"
    ],
    [
      "openalex",
      "2730|Metal complexes synthesis and properties"
    ]
  ],
  "openalex": "W7221315944",
  "pdf_url": "https://pubs.acs.org/inocaj/article-pdf/doi/10.1021/acs.inorgchem.6c02992/68810863/acs.inorgchem.6c02992.pdf",
  "pmcid": "PMC13715578",
  "pmid": "42929613",
  "published": "2026-10-10",
  "publisher": null,
  "ris": "https://research.draconitic.com/paper/a63zk9fbn7bz7.ris",
  "sources": [
    {
      "first_seen": "2026-11-01T12:22:51Z",
      "native_id": "PMC13715578",
      "source": "pmc",
      "url": "https://doi.org/10.1021/acs.inorgchem.6c02992"
    }
  ],
  "subjects": [
    {
      "field": "medicine",
      "origin": "openalex:2730|Metal complexes synthesis and properties",
      "subfield": "oncology"
    }
  ],
  "title": "Synthesis, Cytotoxicity, and Mechanistic Evaluation of Thiazolium-Based Gold(I) Bis‑N‑Heterocyclic Carbene Complexes",
  "title_text": "Synthesis, Cytotoxicity, and Mechanistic Evaluation of Thiazolium-Based Gold(I) Bis‑N‑Heterocyclic Carbene Complexes",
  "type": "peer-reviewed",
  "updated_at": "2026-11-01T12:22:51Z",
  "url": "https://research.draconitic.com/paper/a63zk9fbn7bz7",
  "venue": "Inorganic Chemistry",
  "versions": []
}