Synthesis and initial evaluation of radioactive 5-I-α-methyl-tryptophan: a Trp based agent targeting IDO-1.

A synthetic approach is established to achieve radioactive 5-I-α-methyl-tryptophan (5-I-AMT). An enzyme based assay demonstrated that 5-I-AMT is a substrate of IDO-1. The in vivo distribution and imaging potential of 5-I-AMT were explored with a B16F10 tumor model using I-124 as the radiotag.