{
  "abstract": "Pyrroloquinazolinones, representing the pharmacological scaffold of the natural product Luotonin A, exhibit significant biological activities. Distinguishing from metal-catalysed methodologies, this study delineates a metal-and photocatalystfree strategy for the synthesis of enpyrroloquinazolinone derivatives via a cascade Michael addition-cyclisation-denitrative aromatisation, involving 2-alkynyl quinazolinones and nitroalkenes, which renders the nitro group into a traceless directing group. The resultant enpyrroloquinazolinone analogues underwent systematic evaluation for their anticancer efficacy and potential to activate caspases 3/7 against A549 (NSCLC) and SW480 (colorectal) cancer cell lines. Furthermore, molecular modelling indicates that these enpyrroloquinazolinones possess substantial potential as effective inhibitors of topoisomerase I, providing a promising foundation for the continued development of topoisomerase I inhibitors for therapeutic interventions.",
  "abstract_shown": true,
  "affiliations": [],
  "article_type": null,
  "arxiv": null,
  "author_total": 8,
  "authors": [
    {
      "name": "Han-Kui Wu"
    },
    {
      "name": "Ling Wang"
    },
    {
      "name": "Anjana Patel"
    },
    {
      "name": "William Midgley"
    },
    {
      "name": "Mustapha Musa"
    },
    {
      "name": "Ehmke Pohl"
    },
    {
      "name": "Steven Shnyder"
    },
    {
      "name": "Na Wu",
      "orcid": "0000-0003-1668-6652"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/4d7ns11h97gc2.bib",
  "cited_by": 0,
  "doi": "10.26434/chemrxiv.15009983/v1",
  "fulltext_url": null,
  "id": "4d7ns11h97gc2",
  "issns": [],
  "landing_url": "https://chemrxiv.org/doi/full/10.26434/chemrxiv.15009983/v1",
  "language": null,
  "licence": "CC-BY",
  "licence_label": "CC BY",
  "licence_source": "journal",
  "licence_url": "https://creativecommons.org/licenses/by/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "openalex",
      "1605|Quinazolinone synthesis and applications"
    ]
  ],
  "openalex": "W7220722131",
  "pdf_url": "https://chemrxiv.org/doi/pdf/10.26434/chemrxiv.15009983/v1",
  "pmcid": null,
  "pmid": null,
  "published": "2026-10-06",
  "publisher": "American Chemical Society (ACS)",
  "ris": "https://research.draconitic.com/paper/4d7ns11h97gc2.ris",
  "sources": [
    {
      "first_seen": "2026-10-30T12:17:22Z",
      "native_id": "10.26434/chemrxiv.15009983",
      "source": "chemrxiv",
      "url": "https://chemrxiv.org/doi/full/10.26434/chemrxiv.15009983/v1"
    }
  ],
  "subjects": [
    {
      "field": "chemistry",
      "origin": "openalex:1605|Quinazolinone synthesis and applications",
      "subfield": "organic"
    }
  ],
  "title": "Metal-Free Traceless Directing Group-Assisted Cascade Cyclisation of 2-Alkynylquinazolinones for the Synthesis of Enpyrroloquinazolinones and Their Anticancer Activity",
  "title_text": "Metal-Free Traceless Directing Group-Assisted Cascade Cyclisation of 2-Alkynylquinazolinones for the Synthesis of Enpyrroloquinazolinones and Their Anticancer Activity",
  "type": "preprint",
  "updated_at": "2026-10-30T12:17:22Z",
  "url": "https://research.draconitic.com/paper/4d7ns11h97gc2",
  "venue": "ChemRxiv",
  "versions": []
}