{
  "abstract": "Isocitrate dehydrogenase 1/2 (IDH1/2) mutations are key oncogenic drivers in multiple cancers and represent important diagnostic and therapeutic targets, particularly in glioma and chondrosarcoma. Here, we report the design, synthesis, and in vitro evaluation of iodinated derivatives based on the tetrahydropyrazolopyridine scaffold of the mIDH1 inhibitors SK60 and SK87. Structure-guided modification of the halogenated benzyl moiety yielded iodinated analogues SK140 (9) and SK148 (10), which demonstrated nanomolar inhibitory potencies against IDH1R132C in vitro, exceeding that of the corresponding fluorinated compounds. Radiolabeling was successfully achieved using iodine-125 via organotin precursors, affording [¹²⁵I]SK140 and [¹²⁵I]SK148 in good radiochemical yields. Both radiotracers exhibited excellent stability in formulation media (ethanol, 0.9% NaCl, and PBS) over 24 h at RT. Collectively, these results demonstrate that iodinated tetrahydropyrazolopyridine derivatives can be efficiently radiolabeled and remain stable under formulation conditions, supporting their further evaluation as potential mIDH1-targeting radiotracers.",
  "abstract_shown": true,
  "affiliations": [
    "Research Site Leipzig, Department of Experimental Neurooncological Radiopharmacy, Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Leipzig, Germany.",
    "Faculty of Chemistry and Food Chemistry, School of Science, Technische Universität Dresden, Germany.",
    "Inserm, Imagerie Moléculaire et Stratégies Théranostiques, UMR 1240, Université Clermont Auvergne, Clermont-Ferrand, France.",
    "German Cancer Consortium (DKTK), Partner Site Dresden and German Cancer Research Center (DKFZ), Heidelberg, Germany.",
    "National Center for Tumor Diseases (NCT), NCT/UCC Dresden, a Partnership Between DKFZ Faculty of Medicine and University Hospital Carl Gustav Carus, TUD Dresden University of Technology, and Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Dresden, Germany."
  ],
  "article_type": "research article",
  "arxiv": null,
  "author_total": 8,
  "authors": [
    {
      "affs": [
        0,
        1
      ],
      "name": "Sarandeep Kaur",
      "orcid": "0009-0005-2685-2011"
    },
    {
      "affs": [
        0
      ],
      "name": "Sladjana Dukic-Stefanovic"
    },
    {
      "affs": [
        2
      ],
      "name": "Lucie Arnaud",
      "orcid": "0000-0003-4551-1480"
    },
    {
      "affs": [
        2
      ],
      "name": "Jean-Michel Chezal",
      "orcid": "0000-0001-7162-8450"
    },
    {
      "affs": [
        0
      ],
      "name": "Barbara Wenzel",
      "orcid": "0000-0001-7390-3575"
    },
    {
      "affs": [
        0
      ],
      "name": "Rareş-Petru Moldovan"
    },
    {
      "affs": [
        0,
        1,
        3,
        4
      ],
      "name": "Klaus Kopka",
      "orcid": "0000-0003-4846-1271"
    },
    {
      "affs": [
        2
      ],
      "name": "Aurélie Maisonial-Besset",
      "orcid": "0000-0003-0520-9156"
    }
  ],
  "bibtex": "https://research.draconitic.com/paper/0exzfya8jm8gy.bib",
  "cited_by": 0,
  "doi": "10.1002/jlcr.70039",
  "fulltext_url": "https://europepmc.org/articles/PMC13716505",
  "id": "0exzfya8jm8gy",
  "issns": [
    "0362-4803",
    "1099-1344"
  ],
  "landing_url": "https://europepmc.org/article/MED/42950802",
  "language": "eng",
  "licence": "CC-BY-NC-ND",
  "licence_label": "CC BY-NC-ND",
  "licence_source": "article",
  "licence_url": "https://creativecommons.org/licenses/by-nc-nd/4.0/",
  "metadata_licence": null,
  "native_subjects": [
    [
      "heading",
      "Research Article"
    ],
    [
      "openalex",
      "2741|Radiopharmaceutical Chemistry and Applications"
    ]
  ],
  "openalex": "W7224127794",
  "pdf_url": "https://europepmc.org/articles/PMC13716505?pdf=render",
  "pmcid": "PMC13716505",
  "pmid": "42950802",
  "published": "2026-10-28",
  "publisher": null,
  "ris": "https://research.draconitic.com/paper/0exzfya8jm8gy.ris",
  "sources": [
    {
      "first_seen": "2026-10-31T00:20:33Z",
      "native_id": "MED:42950802",
      "source": "europepmc",
      "url": "https://europepmc.org/article/MED/42950802"
    },
    {
      "first_seen": "2026-11-01T12:23:26Z",
      "native_id": "PMC13716505",
      "source": "pmc",
      "url": "https://doi.org/10.1002/jlcr.70039"
    }
  ],
  "subjects": [
    {
      "field": "medicine",
      "origin": "openalex:2741|Radiopharmaceutical Chemistry and Applications",
      "subfield": "imaging"
    }
  ],
  "title": "Development of Radioiodinated Tetrahydropyrazolopyridine Inhibitors Targeting mIDH.",
  "title_text": "Development of Radioiodinated Tetrahydropyrazolopyridine Inhibitors Targeting mIDH.",
  "type": "peer-reviewed",
  "updated_at": "2026-11-01T12:23:26Z",
  "url": "https://research.draconitic.com/paper/0exzfya8jm8gy",
  "venue": "Journal of labelled compounds & radiopharmaceuticals",
  "versions": []
}