Synthesis and preliminary in vivo evaluation of new [18F]fluoro-inositols as Positron Emission Tomography radiotracers

Publication date: Available online 22 August 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Charlotte Collet, Sébastien Schmitt, Fatiha Maskali, Alexandra Clément, Françoise Chrétien, Gilles Karcher, Pierre-Yves Marie, Sylvain Poussier, Sandrine Lamandé-Langle
This study describes the synthesis and radiosynthesis of eight new [¹⁸F]fluoro-inositol-based radiotracers in myo- and scyllo- inositol configuration. These radiotracers are equipped with a propyl linker bearing fluorine-18. This fluorinated arm is either on a hydroxyl group, i.e. O-alkylated inositols, or on the cyclohexyl backbone, i.e. C-branched derivatives. To modulate lipophilicity, inositols were synthesized in acetylated or hydroxylated form. Automated radiosynthesis was performed on the AllInOne module and the radiotracers were produced in good radiochemical yields (15 to 31.5% dc). Preliminary in vivo preclinical evaluation of these eight [¹⁸F]fluoro-inositols as Positron Emission Tomography (PET) imaging agents in a breast tumour-bearing mouse model was performed and compared with [¹⁸F]-2-fluoro-2-deoxy-D-glucose ([¹⁸F]FDG). Amongst the different inositols, [¹⁸F]myo-2 showed the highest tumour uptake 2.34 ±0.39%ID/g, revealing the potential of this tracer for monitoring breast cancer.

Graphical abstract

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