A Flexible Synthesis of 68Ga-Labeled Carbonic Anhydrase IX (CAIX)-Targeted Molecules via CBT/1,2-Aminothiol Click Reaction

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dc.contributor.authorChen, Kuo-Ting
dc.contributor.authorNguyen, Kevin
dc.contributor.authorIeritano, Christian
dc.contributor.authorGao, Feng
dc.contributor.authorSeimbille, Yann
dc.date.accessioned2020-11-02T20:46:00Z
dc.date.available2020-11-02T20:46:00Z
dc.date.issued2018-12-21
dc.description.abstractWe herein describe a flexible synthesis of a small library of 68Ga-labeled CAIX-targeted molecules via an orthogonal 2-cyanobenzothiazole (CBT)/1,2-aminothiol click reaction. Three novel CBT-functionalized chelators (1–3) were successfully synthesized and labeled with the positron emitter gallium-68. Cross-ligation between the pre-labeled bifunctional chelators (BFCs) and the 1,2-aminothiol-acetazolamide derivatives (8 and 9) yielded six new 68Ga-labeled CAIX ligands with high radiochemical yields. The click reaction conditions were optimized to improve the reaction rate for applications with short half-life radionuclides. Overall, our methodology allows for a simple and efficient radiosynthetic route to produce a variety of 68Ga-labeled imaging agents for tumor hypoxia.en
dc.description.sponsorshipWe gratefully acknowledge the Leenaards Foundation (grant # 3699), NSERC, and the Department of Radiology and Nuclear Medicine at Erasmus MC for financial support.en
dc.identifier.urihttps://doi.org/10.3390/molecules24010023
dc.identifier.urihttp://hdl.handle.net/10012/16489
dc.language.isoenen
dc.publisherMDPIen
dc.rightsAttribution 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/*
dc.subjectcarbonic anhydrase IXen
dc.subject68Ga-labelingen
dc.subjectclick reactionen
dc.subjectcompound libraryen
dc.titleA Flexible Synthesis of 68Ga-Labeled Carbonic Anhydrase IX (CAIX)-Targeted Molecules via CBT/1,2-Aminothiol Click Reactionen
dc.typeArticleen
dcterms.bibliographicCitationChen, K.-T.; Nguyen, K.; Ieritano, C.; Gao, F.; Seimbille, Y. A Flexible Synthesis of 68Ga-Labeled Carbonic Anhydrase IX (CAIX)-Targeted Molecules via CBT/1,2-Aminothiol Click Reaction. Molecules 2019, 24, 23.en
uws.contributor.affiliation1Faculty of Scienceen
uws.contributor.affiliation2Chemistryen
uws.peerReviewStatusRevieweden
uws.scholarLevelPost-Doctorateen
uws.typeOfResourceTexten

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