Synthesis and evaluation of 18F-labeled carbonic anhydrase IX inhibitors for imaging with positron emission tomography

作者：Jinhe Pan, Joseph Lau, Felix Mesak, Navjit Hundal, Maral Pourghiasian, Zhibo Liu, François Bénard, Shoukat Dedhar, Claudiu Trandafir Supuran, Kuo‐Shyan Lin · 发表于：Journal of Enzyme Inhibition and Medicinal Chemistry · 年份：2013 · DOI：10.3109/14756366.2013.773994 · 被引用次数：73 · 研究领域：Enzyme function and inhibition、Synthesis and Catalytic Reactions、Chemical Reactions and Isotopes

Two carbonic anhydrase IX (CA IX) inhibitors were radiolabeled with (18)F, and evaluated for imaging CA IX expression. Despite good affinity for CA IX and excellent plasma stability, uptake of both tracers in CA IX-expressing HT-29 tumor xenografts in mice was low. (18)F-FEC accumulated predominately in the liver and nasal cavity, whereas a significant amount of (18)F-U-104 was retained in blood. Due to minimal uptake in HT-29 tumors compared to other organs/tissues, these two tracers are not suitable for use for CA IX-targeted imaging.