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

被引：62
作者：
Pan, Jinhe [1 ]
Lau, Joseph [1 ]
Mesak, Felix [1 ]
Hundal, Navjit [1 ]
Pourghiasian, Maral [1 ]
Liu, Zhibo [2 ]
Benard, Francois [1 ]
Dedhar, Shoukat [3 ]
Supuran, Claudiu T. [4 ]
Lin, Kuo-Shyan [1 ]
机构：
[1] BC Canc Agcy, Dept Mol Oncol, Vancouver, BC, Canada
[2] Univ British Columbia, Dept Chem, Vancouver, BC, Canada
[3] BC Canc Agcy, Dept Integrat Oncol, Vancouver, BC, Canada
[4] Univ Florence, Lab Chim Bioinorgan, Florence, Italy
来源：
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2014年 / 29卷 / 02期
基金：
加拿大健康研究院;
关键词：
Benzenesulfonamide; coumarin; cytochrome P450; RENAL-CELL CARCINOMA; CYTOCHROMES P450; TUMOR HYPOXIA; EXPRESSION; PET; PROGNOSIS; HEAD; PH; I-131-CG250; SULFONAMIDE;
D O I：
10.3109/14756366.2013.773994
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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. F-18-FEC accumulated predominately in the liver and nasal cavity, whereas a significant amount of F-18-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.
引用
收藏
页码：249 / 255
页数：7
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