Abstract: Cancer belongs to a group of diseases involving abnormal cell growth with the potential to spread to other parts of the body, being currently the leading cause of death worldwide. Cancer therapy is still very challenging and most of the traditional treatments available are usually invasive and cause serious side effects to patients. In this context, photodynamic therapy (PDT) emerges as a good alternative for the treatment of cancer, since it offers great benefits, such as low invasiveness and highly selective. This therapy combines a photosensitizer (PS), light of a specific wavelength, and molecular oxygen (³O₂) to produce reactive oxygen species (ROS), mainly singlet oxygen (¹O₂). Recent studies have shown that Coelenterazine (Clz) and its analogues can be used in PDT exhibiting relevant toxicity to different cancer cells (e.g., breast, liver, prostate, and neuroblastoma) without appreciable harm toward healthy cells. Synthetically, these coumpounds can be obtained from pyrazine units. To develop new photosynthesizers for the application in the PDT, herein we present the synthesis of new pyrazine-based scaffolds to be used for the preparation of novel PS. The different products were characterized by spectroscopy techniques.