期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 1, 页码 324-329出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.10.084
关键词
Radiochemistry; PET; Hypoxia; Click; FMISO
资金
- DIUS
- Siemens Molecular Imaging [TP/16636]
Radiopharmaceuticals for nuclear imaging are essentially targeting molecules, labeled with short-lived radionuclides (e. g., F-18 for PET). A significant drawback of radiopharmaceuticals development is the difficulty to access radiolabeled molecule libraries for initial in vitro evaluation, as radiolabeling has to be optimized for each individual molecule. The present paper discloses a method for preparing libraries of F-18-labeled radiopharmaceuticals using both the fluorous-based F-18-radiochemistry and the Huisgen 1,3-dipolar (click) conjugation reaction. As a proof of concept, this approach allowed us to obtain a series of readily accessible F-18-radiolabeled nitroaromatic molecules, for exploring their structure-activity relationship and further in vitro evaluation of their hypoxic selectivity. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.
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