期刊
ORGANIC & BIOMOLECULAR CHEMISTRY
卷 11, 期 23, 页码 3817-3825出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3ob40548f
关键词
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资金
- Dianne and Irving Kipnes Foundation
- Alberta Innovates - Health Solutions (AIHS)
- Natural Sciences and Engineering Research Council of Canada (NSERC)
The copper-free click chemistry reaction between norbornene and tetrazine species is known to proceed in a rapid, reliable and selective manner under mild conditions. Due to these attractive properties, this reaction has recently been explored as a generally applicable method of bioconjugation. Here, we report a convenient synthetic procedure towards a novel F-18-labelled norbornene derivative ([F-18]NFB) and have evaluated its ability to undergo strain-promoted copper-free click chemistry reactions with two model tetrazine species: an asymmetric dipyridyl tetrazine derivative (Tz) and a tetrazine thiourea-coupled stabilised bombesin peptide (TT-BBN). In both cases, [F-18] NFB was found to undergo rapid and high-yielding click chemistry reactions. Furthermore, as reactions of this type could also potentially be used in vivo to facilitate the development of a novel pretargeting approach for tumour imaging and therapy, we have also assessed the radiopharmacological profile (bioavailability, biodistribution, blood clearance and metabolic stability) of [F-18] NFB in normal BALB/c mice. This radiolabelled compound exhibits both high bioavailability and metabolic stability with approximately 90% remaining intact up to 30 min following administration.
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