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Article Abstract
We herein describe a flexible synthesis of a small library of Ga-labeled CAIX-targeted molecules via an orthogonal 2-cyanobenzothiazole (CBT)/1,2-aminothiol click reaction. Three novel CBT-functionalized chelators (⁻) 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 ( and ) yielded six new Ga-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 Ga-labeled imaging agents for tumor hypoxia.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6337199 | PMC |
| http://dx.doi.org/10.3390/molecules24010023 | DOI Listing |
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