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We hypothesize that FOXM1 inhibitors could represent a novel approach to develop <jats:sup>18<\/jats:sup>F\u2010based radiotracers for Positron Emission Tomography (PET). Therefore, in this report we describe the first attempt to use <jats:sup>18<\/jats:sup>F\u2010labeled FOXM1 inhibitors to detect triple\u2010negative breast cancer (TNBC). Briefly, we replaced the original amide group in the parent drug FDI\u20106 for a ketone group in the novel AF\u2010FDI molecule, to carry out an aromatic nucleophilic (<jats:sup>18<\/jats:sup>F)\u2010fluorination. AF\u2010FDI dissociated the FOXM1\u2010DNA complex, decreased FOXM1 levels, and inhibited cell proliferation in a TNBC cell line (MDA\u2010MB\u2010231). [<jats:sup>18<\/jats:sup>F]AF\u2010FDI was internalized in MDA\u2010MB\u2010231 cells. Cell uptake inhibition experiments showed that AF\u2010FDI and FDI\u20106 significantly decreased the maximum uptake of [<jats:sup>18<\/jats:sup>F]AF\u2010FDI, suggesting specificity towards FOXM1. [<jats:sup>18<\/jats:sup>F]AF\u2010FDI reached a tumor uptake of SUV=0.31 in MDA\u2010MB\u2010231 tumor\u2010bearing mice and was metabolically stable 60\u2005min post\u2010injection. These results provide preliminary evidence supporting the potential role of FOXM1 to develop PET radiotracers.<\/jats:p>","DOI":"10.1002\/cmdc.202100279","type":"journal-article","created":{"date-parts":[[2021,8,17]],"date-time":"2021-08-17T01:07:21Z","timestamp":1629162441000},"page":"3720-3729","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["FOXM1 Inhibitors as Potential Diagnostic Agents: First Generation of a PET Probe Targeting FOXM1 To Detect Triple\u2010Negative Breast Cancer <i>in\u2005vitro<\/i> and <i>in\u2005vivo<\/i>"],"prefix":"10.1002","volume":"16","author":[{"given":"David J.","family":"P\u00e9rez","sequence":"first","affiliation":[{"name":"Faculty of Pharmacy and Pharmaceutical Sciences University of Alberta  Edmonton AB, T6E 2E1 Canada"},{"name":"Facultad de Medicina, Unidad de Radiofarmacia\/ciclotr\u00f3n Universidad Nacional Aut\u00f3noma de M\u00e9xico  Ciudad de M\u00e9xico C.P. 04510 CDMX Mexico"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Seyed","family":"Amirhossein Tabatabaei Dakhili","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy and Pharmaceutical Sciences University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Cody","family":"Bergman","sequence":"additional","affiliation":[{"name":"Department of Oncology, Faculty of Medicine and Dentistry University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jennifer","family":"Dufour","sequence":"additional","affiliation":[{"name":"Department of Oncology, Faculty of Medicine and Dentistry University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Melinda","family":"Wuest","sequence":"additional","affiliation":[{"name":"Department of Oncology, Faculty of Medicine and Dentistry University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Freimut D.","family":"Juengling","sequence":"additional","affiliation":[{"name":"Department of Oncology, Faculty of Medicine and Dentistry University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Frank","family":"Wuest","sequence":"additional","affiliation":[{"name":"Department of Oncology, Faculty of Medicine and Dentistry University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Carlos A.","family":"Vel\u00e1zquez\u2010Mart\u00ednez","sequence":"additional","affiliation":[{"name":"Faculty of Pharmacy and Pharmaceutical Sciences University of Alberta  Edmonton AB, T6E 2E1 Canada"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2021,10,22]]},"reference":[{"key":"e_1_2_7_1_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bbagrm.2011.09.004"},{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.semcancer.2017.08.009"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1517\/13543780903563364"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.4161\/15384047.2014.987566"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1038\/ncomms6165"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41419-017-0156-7"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.1126\/scisignal.aai8583"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jmgm.2018.01.009"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2019.103269"},{"key":"e_1_2_7_10_1","first-page":"87","volume":"54","author":"Yanli T.","year":"2019","journal-title":"Int. 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