As we all know, cancer is still a disease that we are struggling against. Although the traditional treatment is still the mainstream in clinical practice, the emerging phototheranostics technologies based on photoacoustic or fluorescence imaging–guided phototherapy also provide a new exploration direction for the non-invasive, low-risk and highly efficient cancer treatment. Photosensitizer is the core material to accomplish this mission. Recently, more attention has been paid to the emerging A−D−A fused-ring photosensitizers. A−D−A fused-ring photosensitizers display strong and wide absorption spectra, high photostability and easy molecular modification. Since such kind of photosensitizers was firstly used for tumor therapy in 2019, their application boundaries are constantly expanding. Therefore, in this feature article, from the perspective of molecular design, we focused on the development of these molecules in phototheranostics over the past five years. The effects of tiny structural changes on their photophysical properties are discussed in detail, which provides a way for structural optimization of the subsequent A−D−A photosensitizers.

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