Medical Application of In-cell Reactions with Acrolein in Cancer

We recently discovered that acrolein is produced at high concentrations in various cancer cells. We then developed an efficient in-cell reaction with acrolein in cancer; thus, the aryl azides undergo a metal-free 1,3-dipolar cycloaddition reaction with acrolein in a highly selective manner, resulting in the formation of α-diazocarbonyl derivatives. In this paper, we describe our recent trials of this in-cell reaction toward medical applications, i.e., cancer diagnosis and therapy. Our in-cell reaction strategy led to the clinical application and constitutes a new modality for cancer medicine.