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

页码：249 / 255

页数：7

共 50 条

[31] In vivo biodistribution and pharmacokinetics of 18F-labeled human C-peptide:: evaluation in monkeys using positron emission tomography
Fredriksson, A
Ekberg, K
Ingvar, M
Johansson, BL
Wahren, J
Stone-Elander, S
LIFE SCIENCES, 2002, 71 (12) : 1361 - 1370
[32] Evaluation of a Novel 18F-Labeled Positron-Emission Tomography Perfusion Tracer for the Assessment of Myocardial Infarct Size in Rats
Sherif, Hossam M.
Saraste, Antti
Weidl, Eliane
Weber, Axel W.
Higuchi, Takahiro
Reder, Sybille
Poethko, Thorsten
Hemiksen, Gjermund
Casebier, David
Robinson, Simon
Wester, Hans-Juergen
Nekolla, Stephan G.
Schwaiger, Markus
CIRCULATION-CARDIOVASCULAR IMAGING, 2009, 2 (02) : 77 - 84
[33] Design, Synthesis, and Evaluation of an 18F-Labeled Radiotracer Based on Celecoxib-NBD for Positron Emission Tomography (PET) Imaging of Cyclooxygenase-2 (COX-2)
Kaur, Jatinder
Tietz, Ole
Bhardwaj, Atul
Marshall, Alison
Way, Jenilee
Wuest, Melinda
Wuest, Frank
CHEMMEDCHEM, 2015, 10 (10) : 1635 - 1640
[34] Synthesis and Evaluation of Three 18F-Labeled Aminophenylbenzothiazoles as Amyloid Imaging Agents
Serdons, Kim
Van Laere, Koen
Janssen, Peter
Kung, Hank F.
Bormans, Guy
Verbruggen, Alfons
JOURNAL OF MEDICINAL CHEMISTRY, 2009, 52 (22) : 7090 - 7102
[35] Synthesis and Evaluation of 18F-Labeled Peptide for Gonadotropin-Releasing Hormone Receptor Imaging
Huang, Shun
Li, Hongsheng
Han, Yanjiang
Fu, Lilan
Ren, Yunyan
Zhang, Yin
Li, Youcai
Sun, Penghui
Wang, Meng
Wu, Hubing
Wang, Quanshi
Hu, Kongzhen
CONTRAST MEDIA & MOLECULAR IMAGING, 2019,
[36] Novel 18F-Labeled Isonicotinamide-Based Radioligands for Positron Emission Tomography Imaging of Glycogen Synthase Kinase-3β
Zhong, Yuhua
Yang, Shaoxi
Cui, Jianyu
Wang, Jie
Li, Lin
Chen, Yilin
Chen, Junjie
Feng, Pengju
Huang, Shun
Li, Hongsheng
Han, Yanjian
Tang, Ganghua
Hu, Kongzhen
MOLECULAR PHARMACEUTICS, 2021, 18 (03) : 1277 - 1284
[37] Synthesis and SAR of Novel Re/99mTc-Labeled Benzenesulfonamide Carbonic Anhydrase IX Inhibitors for Molecular Imaging of Tumor Hypoxia
Lu, Genliang
Hillier, Shawn M.
Maresca, Kevin P.
Zimmerman, Craig N.
Eckelman, William C.
Joyal, John L.
Babich, John W.
JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (02) : 510 - 520
[38] Synthesis and Evaluation of 18F-Labeled Styryltriazole and Resveratrol Derivatives for β-Amyloid Plaque Imaging
Lee, Iljung
Choe, Yearn Seong
Choi, Joon Young
Lee, Kyung-Han
Kim, Byung-Tae
JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (02) : 883 - 892
[39] Novel 18F-Labeled Benzoxazole Derivatives as Potential Positron Emission Tomography Probes for Imaging of Cerebral β-Amyloid Plaques in Alzheimer's Disease
Cui, Mengchao
Ono, Masahiro
Kimura, Hiroyuki
Ueda, Masashi
Nakamoto, Yuji
Togashi, Kaori
Okamoto, Yoko
Ihara, Masafumi
Takahashi, Ryosuke
Liu, Boli
Saji, Hideo
JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (21) : 9136 - 9145
[40] Synthesis and Biological Evaluation of 18F-Labeled Fluoroethoxy Tryptophan Analogues as Potential PET Tumor Imaging Agents
Chiotellis, Aristeidis
Muller, Adrienne
Mu, Linjing
Keller, Claudia
Schibli, Roger
Kraemer, Stefanie D.
Ametamey, Simon M.
MOLECULAR PHARMACEUTICS, 2014, 11 (11) : 3839 - 3851

← 1 2 3 4 5 →