Synthesis and evaluation of 18F-labeled tertiary benzenesulfonamides for imaging carbonic anhydrase IX expression in tumours with positron emission tomography

被引：19

作者：

Lau, Joseph ^{[1
]}

Pan, Jinhe ^{[1
]}

Zhang, Zhengxing ^{[1
]}

Hundal-Jabal, Navjit ^{[1
]}

Liu, Zhibo ^{[2
]}

Benard, Francois ^{[1
]}

Lin, Kuo-Shyan ^{[1
]}

机构：

[1] BC Canc Agcy, Dept Mol Oncol, Vancouver, BC V5Z 1L3, Canada

[2] Univ British Columbia, Dept Chem, Vancouver, BC V6T 1Z1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 14期

基金：

加拿大健康研究院;

关键词：

Carbonic anhydrase IX; Tertiary benzenesulfonamides; Fluorine-18; In vivo defluorination; Positron emission tomography; RENAL-CELL CARCINOMA; CA-IX; BREAST-CANCER; PROGNOSTIC-SIGNIFICANCE; SURROGATE MARKER; IN-VITRO; HYPOXIA; INHIBITORS; PET; PH;

D O I：

10.1016/j.bmcl.2014.05.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three tertiary benzenesulfonamide inhibitors 4a-c were radiolabeled with F-18 and evaluated for imaging carbonic anhydrase IX (CA IX) expression with positron emission tomography. All three inhibitors exhibit <10 nM affinity for CA IX with no measurable affinity for CA II. Despite good affinity/selectivity to CA IX and excellent stability in plasma, uptake of [F-18]4a-c in CA IX-expressing HT-29 tumours was low without significant contrast. [F-18]4a,b were excreted rapidly, while [F-18]4c exhibited significant in vivo defluorination leading to high bone uptake. Due to minimal uptake in HT-29 tumours compared to normal organs/tissues, F-18-labeled benzenesulfonamides [F-18]4a-c are not suitable as CA IX imaging agents. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：3064 / 3068

页数：5

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