Four fac-[Re(CO)₃(phen)(L)] complexes with phen = 1,10-phenanthroline and L = a non-steroidal anti-inflammatory drug (NSAID) carboxylate ligand were obtained from the reaction of fac-[ReCl(CO)₃(phen)] with ligands such as aspirin, (S)-(+)-ibuprofen, (S)-(+)-naproxen and indomethacin. Single-crystal X-ray diffraction analysis revealed a pseudo-octahedral coordination of the rhenium atom whereas the NSAID carboxylates act as monodentate ligands. The complexes show orange luminescence in polar solvents. Of the four compounds obtained, only fac-[Re(CO)₃(phen)(aspirin)] exhibited activity against HeLa human cancer cells while it was inactive against the non-tumorigenic mouse L929 cell line. After uptake and dissociation in HeLa cells, the fac-[Re(CO)₃(phen)(aspirin)] complex produces the luminescent fac-[Re(CO)₃(phen)]⁺ cation, which predominantly accumulates in the mitochondria but does not penetrate to the nucleus, as shown by confocal microscopy. Once generated, the fac-[Re(CO)₃(phen)]⁺ cation reversibly binds to hen egg white lysozyme (HEWL) while the aspirin ligand holds the ability to inhibit the COX-2 enzyme. The anticancer activity of the fac-[Re(CO)₃(phen)(aspirin)] complex could be linked to ROS production, and cell cycle disturbance followed by triggering an apoptotic pathway of cell death.

中文翻译：

---

发光的fac- [Re（CO）₃（phen）]羧基与非甾体类抗炎药的复合物：fac- [Re（CO）₃（phen）（阿司匹林））体外抗癌活性的合成和机理研究†

四个FAC - [的Re（CO）₃（phen）的（L）]与苯= 1,10-菲咯啉和L络合物=从的反应得到的非甾体抗炎药（NSAID）羧酸酯配体FAC - [ ReCl（CO）₃（phen）]与阿司匹林，（S）-（+）-布洛芬，（S）-（+）-萘普生和消炎痛等配体。单晶X射线衍射分析显示the原子的拟八面体配位，而NSAID羧酸盐起单齿配体的作用。该配合物在极性溶剂中显示出橙色发光。在获得的四种化合物中，只有fac- [Re（CO）₃（phen）（阿司匹林）对HeLa人类癌细胞具有活性，而对非致瘤性小鼠L929细胞系则无活性。在HeLa细胞中摄取并解离后，fac- [Re（CO）₃（phen）（阿司匹林）]复合物产生发光的fac- [Re（CO）₃（phen）] ⁺阳离子，其主要堆积在线粒体中，但如共聚焦显微镜所示，它不会穿透细胞核。一旦生成，fac- [Re（CO）₃（phen）] ⁺阳离子可逆地结合于鸡蛋清溶菌酶（HEWL），而阿司匹林配体则具有抑制COX-2酶的能力。FAC的抗癌活性-[Re（CO）₃（phen）（阿司匹林）]复合物可能与ROS的产生有关，并且细胞周期紊乱随后触发了细胞死亡的凋亡途径。