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Synthesis and Biological Evaluation of a New Acyclic Pyrimidine Derivative as a Probe for Imaging Herpes Simplex Virus Type 1 Thymidine Kinase Gene Expression

With the idea of finding a more selective radiotracer for imaging herpes simplex virus type 1 thymidine kinase (HSV1-tk) gene expression by means of positron emission tomography (PET), a novel [18F]fluorine radiolabeled pyrimidine with 4-hydroxy-3- (hydroxymethyl)butyl side chain at N-1 (HHB-5- [18F]FEP) was prepared and evaluated as a potential PET probe. Unlabeled reference compound, HHB-5-FEP, was synthesized via a five-step reaction sequence starting from 5-(2- acetoxyethyl)-4-methoxypyrimidin- 2-one. The radiosynthesis of HHB-[18F]-FEP was accomplished by nucleophilic radiofluorination of a tosylate precursor using [18F]fluoride- cryptate complex in 45% ± 4 (n = 4) radiochemical yields and high purity (> 99%). The biological evaluation indicated the feasibility of using HHB-5-[18F]FEP as a PET radiotracer for monitoring HSV1-tk expression in vivo.

acyclic pyrimidine nucleoside analogues ; PCV-like side chain ; fluorination ; radiosynthesis ; positron emission tomography (PET) ; HSV1-TK

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