Liang Hong-Yu, Jiang Ying, Yan Yi-Jia, Wang Lu-Qi, Chen Pei-Ran, Chen Zhi-Long
Department of Pharmaceutical Science & Technology, Donghua University, Shanghai 201620, China.
Department of Pharmacy, Huadong Hospital, Fudan University, Shanghai 200040, China.
ACS Omega. 2025 Mar 11;10(11):11119-11127. doi: 10.1021/acsomega.4c10221. eCollection 2025 Mar 25.
To discover a potential anticancer photosensitizer drug, a series of -tetraphenyltetrabenzoporphyrins (-PhTBPs) with four carboxyl groups were afforded through a multistep reaction starting from cyclohexene. These new -PhTBPs demonstrated favorable antiaggregation properties and exhibited obvious absorption in the phototherapeutic window (600-800 nm). Additionally, -PhTBPs 1-5 displayed notable reactive oxygen species generation ability and obvious photodamage effectiveness against Eca-109 cells. Furthermore, -PhTBP 4 was able to inhibit tumor growth in mice bearing Eca-109 cells and demonstrated superior biosafety toward the kidney and liver both and . These results indicated that compound 4 could be considered a promising candidate for further studies in photodynamic therapy.
为发现一种潜在的抗癌光敏剂药物，通过从环己烯开始的多步反应制备了一系列带有四个羧基的-四苯基四苯并卟啉（-PhTBPs）。这些新型-PhTBPs表现出良好的抗聚集性能，并在光疗窗口（600 - 800 nm）有明显吸收。此外，-PhTBPs 1 - 5展现出显著的活性氧生成能力以及对Eca - 109细胞明显的光损伤效果。此外，-PhTBP 4能够抑制携带Eca - 109细胞的小鼠体内肿瘤生长，并且在体内和体外对肾脏和肝脏均表现出优异的生物安全性。这些结果表明化合物4可被视为光动力疗法进一步研究的有前景的候选物。
