As a group of heterocyclic macrocycle organic natural compounds occurring universally in
animal tissues and plants, porphyrins are composed of four modified pyrrole subunits. Porphyrin analogues/
derivatives possess multiple biochemical properties because of their unique structures and have
been extensively investigated in cancer treatment. Studies have shown that porphyrins and their derivatives
have the ability to locate tumor cells in a variety of human cancers, and these compounds not
only exhibit potent therapeutic effects as photodynamic agents but also show promising properties in
medicinal imaging, such as MRI, photoacoustic imaging, fluorescence imaging, and PET/SPECT imaging.
This paper reviews the recent reports of porphyrin derivatives as therapeutic agents used in tumor
therapies, such as sonodynamic therapy, photodynamic therapy and radiotherapy, as well as the
imaging agents for multimodality tumor imaging. The limitations of porphyrin-based compounds in
tumor treatments and future prospects are also summarized.