An HSP90 inhibitor based fluorescent probe for selective tumor targeting

Fluorescent imaging has been widely used in the detection of diseases, especially cancer. Among them, biomarker-specific ligand-based imaging strategies have attracted much attention, due to their improved image contrast and diagnostic accuracy. In this work, an HSP90 inhibitor based fluorescent probe (Probe 1) was synthesized possessing the potential of selective tumor targeting, which was constructed with an HSP90 inhibitor and 4-hydroxy-1,8-naphthalimide derivative. Probe 2, a resorcinol-blocked probe was also synthesized as a control, which prevented binding with the HSP90 ATP binding pocket. Biological studies showed that Probe 1 could be selectively accumulated by tumor cells, while Probe 2 not, suggesting that Probe 1 is a promising targeted tumor imaging agent for early diagnosis.