{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,1]],"date-time":"2026-10-01T02:49:35Z","timestamp":1790822975287,"version":"4.1.0"},"reference-count":40,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2022,6,11]],"date-time":"2022-06-11T00:00:00Z","timestamp":1654905600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"European Regional Development Fund (ERDF) and the Free State of Saxony, Germany","award":["100364142"],"award-info":[{"award-number":["100364142"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Isocitrate dehydrogenases (IDHs) are metabolic enzymes commonly mutated in human cancers (glioma, acute myeloid leukaemia, chondrosarcoma, and intrahepatic cholangiocarcinoma). These mutated variants of IDH (mIDH) acquire a neomorphic activity, namely, conversion of \u03b1-ketoglutarate to the oncometabolite D-2-hydroxyglutarate involved in tumourigenesis. Thus, mIDHs have emerged as highly promising therapeutic targets, and several mIDH specific inhibitors have been developed. However, the evaluation of mIDH status, currently performed by biopsy, is essential for patient stratification and thus treatment and follow-up. We report herein the development of new radioiodinated and radiofluorinated analogues of olutasidenib (FT-2102) as tools for noninvasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging of mIDH1 up- and dysregulation in tumours. Nonradiolabelled derivatives 2 and 3 halogenated at position 6 of the quinolinone scaffold were synthesised and tested in vitro for their inhibitory potencies and selectivities in comparison with the lead compound FT-2102. Using a common organotin precursor, (S)-[125I]2 and (S)-[18F]3 were efficiently synthesised by radio-iododemetallation and copper-mediated radiofluorination, respectively. Both radiotracers were stable at room temperature in saline or DPBS solution and at 37 \u00b0C in mouse serum, allowing future planning of their in vitro and in vivo evaluations in glioma and chondrosarcoma models.<\/jats:p>","DOI":"10.3390\/molecules27123766","type":"journal-article","created":{"date-parts":[[2022,6,12]],"date-time":"2022-06-12T22:37:20Z","timestamp":1655073440000},"page":"3766","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["Novel Radioiodinated and Radiofluorinated Analogues of FT-2102 for SPECT or PET Imaging of mIDH1 Mutant Tumours"],"prefix":"10.3390","volume":"27","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-4752-631X","authenticated-orcid":false,"given":"Val\u00e9rie","family":"Weber","sequence":"first","affiliation":[{"name":"Universit\u00e9 Clermont Auvergne, Inserm, Imagerie Mol\u00e9culaire et Strat\u00e9gies Th\u00e9ranostiques, UMR 1240, F-63000 Clermont-Ferrand, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4551-1480","authenticated-orcid":false,"given":"Lucie","family":"Arnaud","sequence":"additional","affiliation":[{"name":"Universit\u00e9 Clermont Auvergne, Inserm, Imagerie Mol\u00e9culaire et Strat\u00e9gies Th\u00e9ranostiques, UMR 1240, F-63000 Clermont-Ferrand, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sladjana","family":"Dukic-Stefanovic","sequence":"additional","affiliation":[{"name":"Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, 04318 Leipzig, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7390-3575","authenticated-orcid":false,"given":"Barbara","family":"Wenzel","sequence":"additional","affiliation":[{"name":"Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, 04318 Leipzig, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0404-2892","authenticated-orcid":false,"given":"Val\u00e9rie","family":"Roux","sequence":"additional","affiliation":[{"name":"Universit\u00e9 Clermont Auvergne, Inserm, Imagerie Mol\u00e9culaire et Strat\u00e9gies Th\u00e9ranostiques, UMR 1240, F-63000 Clermont-Ferrand, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7162-8450","authenticated-orcid":false,"given":"Jean-Michel","family":"Chezal","sequence":"additional","affiliation":[{"name":"Universit\u00e9 Clermont Auvergne, Inserm, Imagerie Mol\u00e9culaire et Strat\u00e9gies Th\u00e9ranostiques, UMR 1240, F-63000 Clermont-Ferrand, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8157-8979","authenticated-orcid":false,"given":"Thu-Hang","family":"Lai","sequence":"additional","affiliation":[{"name":"Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, 04318 Leipzig, Germany"},{"name":"Department of Research and Development, ROTOP Pharmaka GmbH, 01328 Dresden, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Rodrigo","family":"Teodoro","sequence":"additional","affiliation":[{"name":"Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, 04318 Leipzig, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4846-1271","authenticated-orcid":false,"given":"Klaus","family":"Kopka","sequence":"additional","affiliation":[{"name":"Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, 04318 Leipzig, Germany"},{"name":"Technical University Dresden, School of Science, Faculty of Chemistry and Food Chemistry, 01062 Dresden, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elisabeth","family":"Miot-Noirault","sequence":"additional","affiliation":[{"name":"Universit\u00e9 Clermont Auvergne, Inserm, Imagerie Mol\u00e9culaire et Strat\u00e9gies Th\u00e9ranostiques, UMR 1240, F-63000 Clermont-Ferrand, France"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3168-3062","authenticated-orcid":false,"given":"Winnie","family":"Deuther-Conrad","sequence":"additional","affiliation":[{"name":"Helmholtz-Zentrum Dresden-Rossendorf, Institute of Radiopharmaceutical Cancer Research, Research Site Leipzig, 04318 Leipzig, Germany"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0520-9156","authenticated-orcid":false,"given":"Aur\u00e9lie","family":"Maisonial-Besset","sequence":"additional","affiliation":[{"name":"Universit\u00e9 Clermont Auvergne, Inserm, Imagerie Mol\u00e9culaire et Strat\u00e9gies Th\u00e9ranostiques, UMR 1240, F-63000 Clermont-Ferrand, France"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,6,11]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"37","DOI":"10.1186\/s13578-017-0165-3","article-title":"Isocitrate Dehydrogenases in Physiology and Cancer: Biochemical and Molecular Insight","volume":"7","year":"2017","journal-title":"Cell Biosci."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"730","DOI":"10.1158\/2159-8290.CD-13-0083","article-title":"Oncogenic Isocitrate Dehydrogenase Mutations: Mechanisms, Models, and Clinical Opportunities","volume":"3","author":"Cairns","year":"2013","journal-title":"Cancer Discov."},{"key":"ref_3","doi-asserted-by":"crossref","first-page":"599","DOI":"10.1093\/annonc\/mdw013","article-title":"IDH Mutations in Cancer and Progress toward Development of Targeted 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