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MOLECULAR DIVERSITY · 2025 · IF 3.8

Synthesis of porphyrin-formononetin derivatives and their anti-tumor activity studies

Yang Lingyan,He Shan,Tang Chen,Shi Lei,Liu Zhenhua,Tian Zejie,Li Hui,He Xufeng,Liao Jiding,Liu Yunmei

Photodynamic therapy (PDT) has received much attention in cancer treatment because of its low toxicity and side effects. In this study, we successfully synthesized 14 novel porphyrin-formononetin derivatives. In reactive oxygen species detection experiments, the target compounds 4a–6d caused a significant decrease in the fluorescence intensity of DPBF compared with the porphyrin parent and formononetin feedstock after illumination, and it was found that the target compound had a higher ROS quantum yield, among which the quantum yield of compound 6c was higher. In the in vitro anti-tumor activity assay, the target compounds 4a–6d exhibited a certain degree of growth inhibition against six cancer cells (A549, MDA-MB-231, HCT-116, HGC-27, DU145, and TCCSUP) under light conditions, whereas the cytotoxicity of the target compounds against the normal cells H9c2 was less. The results of the scratch assay showed that 6c could inhibit the growth of tumor cells by inhibiting the migration of DU145 cells. The experimental results indicate that the target compounds achieve the synergistic effect of PDT and chemotherapy. Graphical abstract

研究领域: 药理学 · 肿瘤学 · 有机化学
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