Synthesis and biological evaluation of (18)F-labeled Fluoroethoxy tryptophan analogues as potential PET tumor imaging agents

Chiotellis, Aristeidis; Muller, Adrienne; Mu, Linjing; Keller, Claudia; Schibli, Roger; Krämer, Stefanie D; Ametamey, Simon M

doi:10.1021/mp500312t

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Chiotellis, A., Muller, A., Mu, L., Keller, C., Schibli, R., Krämer, S. D., & Ametamey, S. M. (2014). Synthesis and biological evaluation of (18)F-labeled Fluoroethoxy tryptophan analogues as potential PET tumor imaging agents. Molecular Pharmaceutics, 11(11), 3839–3851. https://doi.org/10.1021/mp500312t

Abstract

As a continuation of our research efforts toward the development of tryptophan-based radiotracers for tumor imaging with positron emission tomography (PET), three new fluoroethoxy tryptophan analogues were synthesized and evaluated in vivo. These new tracers (namely, 4-(2-[(18)F]fluoroethoxy)-dl-tryptophan ([(18)F]4-FEHTP), 6-(2-[(18)F]fluoroethoxy)-dl-tryptophan ([(18)F]6-FEHTP), and 7-(2-[(18)F]fluoroethoxy)-dl-tryptophan ([(18)F]7-FEHTP) carry the fluoroethoxy side chain either at positions 4-, 6-, or 7- of the indole core. Referen