A series of novel symmetric or unsymmetric silicon (IV) phthalocyanines axially substituted with cyclic Arg-Gly-Asp (cRGD) ligands through different ethylene glycol chains have been synthesized by a facile and mild “click” reaction. All the compounds show efficient photosensitizing activities in N,N-dimethylformamide, and are essentially non-aggregated in RPMI 1640 medium with 0.05% Cremophor EL. Owing to the presence of two cRGD ligands, the conjugate 6b exhibits highest selectivity toward α_vβ₃⁺ HT-29 cells in photocytotoxicities. It shows higher cellular uptake and ROS generation efficiency toward the α_vβ₃⁺ HT-29 cells compared with that of α_vβ₃^- MCF-7 cells. The competitive cellular uptake and subcellular localization indicate that 6b is internalized mainly through integrin-mediated endocytosis. In addition, the in vivo studies showed that 6b can mainly accumulate in tumor sites and show a significant PDT effect resulting in 75% tumor growth inhibition. The results indicate that 6b is a highly promising photosensitizer for targeted photodynamic therapy.

通过简便且温和的“喀哒”反应合成了一系列新颖的对称或非对称硅（IV）酞菁，它们通过不同的乙二醇链轴向被环状Arg-Gly-Asp（cRGD）配体取代。所有化合物在N，N-二甲基甲酰胺中均显示出有效的光敏活性，并且在含有0.05％Cremophor EL的RPMI 1640培养基中基本上没有聚集。由于2个的cRGD配体的存在下，所述缀合物6B表现出最高的选择性朝向α _v β ₃ ⁺ HT-29细胞在photocytotoxicities。它显示出更高的细胞摄取和ROS产生的效率朝向α _v β ₃ ⁺HT-29细胞与α相比_v β ₃ ^- MCF-7细胞。竞争性细胞摄取和亚细胞定位表明6b主要是通过整合素介导的内吞作用而被内在化的。此外，体内研究表明6b可以主要在肿瘤部位积聚，并显示出显着的PDT效应，导致75％的肿瘤生长受到抑制。结果表明6b是用于靶向光动力疗法的高度有前途的光敏剂。