Improved IR780 derivatives bearing morpholine group as tumor-targeted therapeutic agent for near-infrared fluorescence imaging and photodynamic therapy

To improve of the potency of IR780 in this field of anticancer research, we designed and synthesized two novel IR780-based derivatives (L-1 and L-2) possessing different chainlength tethered morpholine groups. Their properties were verified through both in vitro and in vivo experiments, including good photo- and chemical stability, dual tumor-targeted property, and near-infrared fluorescence imaging and targeted PDT. Meanwhile, L-1 was further verified for potential practicability, including the hypotoxicity and the mixed route of elimination from the body, through the in vivo experiment. All results show that that our tactics provide a protocol for improvement of the potency of IR780 in the field of anticancer research.