Radiolabelling and evaluation of a novel sulfoxide as a PET imaging agent for tumor hypoxia

Abstract

[18F]FMISO is the most widely validated PET radiotracer for imaging hypoxic tissue. However, as a result of the pharmacokinetics of [18F]FMISO a 2h wait between tracer administration and patient scanning is required for optimal image acquisition. In order to develop hypoxia imaging agents with faster kinetics, we have synthesised and evaluated several F-18 labelled anilino sulfoxides. In this manuscript we report on the synthesis, in vitro and in vivo evaluation of a novel fluoroethyltriazolyl propargyl anilino sulfoxide. The radiolabelling of the novel tracer was achieved via 2-[18F]fluoroethyl azide click chemistry. Radiochemical yields were 23±4% based on 2-[18F]fluoroethyl azide and 7±2%..