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Synthesis and in vitro evaluation of 18F labeled tyrosine derivatives as potential positron emission tomography (PET) imaging agents

Authors:	Limin Wang Wenchao Qu Brian Lieberman Karl Ploessl Hank F. Kung

Affiliation:	1. Department of Chemistry, University of Pennsylvania, Philadelphia, PA 19104, United States;2. Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, United States;3. Department of Pharmacology, University of Pennsylvania, Philadelphia, PA 19104, United States

Abstract:	Three new ¹⁸F labeled fluoroalkyl tyrosine derivatives, O-(2-[¹⁸F]fluoroethyl)-α-methyltyrosine (FEMT, [¹⁸F]2), O-(2-[¹⁸F]fluoroethyl)-2-l-azatyrosine (FEAT, [¹⁸F]3), O-(2-[¹⁸F]fluoroethyl)-l-tyrosineamide (FETA, [¹⁸F]4) have been synthesized and radiofluorinated with 5–34% decay-corrected yield. In vitro studies were carried out in U-138 MG human glioblastoma. Cellular uptake of new tracers was compared to clinically utilized imaging agent O-(2-[¹⁸F]fluoroethyl)-l-tyrosine (FET, [¹⁸F]1). The uptake of tracers followed the order of FET ([¹⁸F]1) > FEAT([¹⁸F]3) > FEMT ([¹⁸F]2) ≈ FETA ([¹⁸F]4).

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