Three novel 17³-dicarboxylethyl-pyropheophorbide-a amide derivatives as photosensitizers for photodynamic therapy (PDT) were synthesized from pyropheophorbide-a (Ppa). Their photophysical and photochemical properties, intracellular localization, photocytotoxicity in vitro and in vivo were investigated. All target compounds exhibited low cytotoxicity in the dark and remarkable photocytotoxicity against human esophageal cancer cells. Among them, 1a showed highest singlet oxygen quantum yield. Upon light activation, 1a exhibited significant photocytotoxicity. After PDT treatment, the growth of Eca-109 tumor in nude mice was significantly inhibited. Therefore, 1a is a powerful and promising antitumor photosensitizer for PDT.

从焦脱镁叶绿酸-a（Ppa）合成了三种新型的17 ^3-二羧乙基-焦脱镁叶绿酸-a酰胺衍生物作为光动力疗法（PDT）的光敏剂。研究了它们在体外和体内的光物理和光化学特性，细胞内定位，光细胞毒性。所有目标化合物在黑暗中均显示出低细胞毒性，并且对人食道癌细胞具有显着的光细胞毒性。其中，1a表现出最高的单线态氧量子产率。光激活后，1a表现出明显的光细胞毒性。PDT处理后，裸鼠中Eca-109肿瘤的生长受到明显抑制。因此，1a 是用于PDT的强大而有前途的抗肿瘤光敏剂。